ABSTRACT

Targeted drug delivery, also known as smart drug delivery, is a method of treatment that involves the increase in medicament in one or few body parts in comparison to others. Two strategies are widely used for drug targeting to the desired organ/tissue: passive targeting and active targeting. Drug delivery vehicles transport the drug either within or in the vicinity of target. An ideal drug delivery vehicle is supposed to cross even stubborn sites such as a blood brain barrier. Recently, nano medicine has emerged as the medical application of nanotechnology. Since nanoparticles are very small in size, nano drug delivery can allow for the delivery of drugs with poor solubility in water and also aid in avoiding the first pass metabolism of liver. Nanotechnology derived drug delivery can cause the drug to remain in blood circulation for a long time, thereby leading to lesser fluctuations in plasma levels and therefore, minimal side effects. These include polymer-drug conjugates and nano particulate systems such as liposomes, quantum dots, dendrimers, etc. There are several other approaches as well. These also include the strategies wherein the therapeutic agents are coupled with “targeting ligands” that possess the ability to recognize antigens associated with tumors.

Keywords: Targeted drug delivery, Nanoparticles, Therapeutic, Conjugates, Cancer, Release.

ABSTRACT

Unani system of medicine recognizes the influence of surroundings and ecological conditions on the state of health of human beings. This system aims at restoring the equilibrium of various elements and faculties of the human body. It has laid down six essential pre-requisites for the prevention of diseases and places great emphasis, on the maintenance of proper ecological balance and, on the other, on keeping water, food and air free from pollution. These essentials, known as 'Asbab-e-Sitta Zarooriya' and are as follows, air, food and drinks, bodily movement and repose, psychic movement and repose, sleep and wakefulness, and exertion and retention etc. In this article we will discuss on these six essentials, how they play an important role in preservation of health and how these are correlated with tabiat in maintenance of health.

Keywords: six essentials, food and drinks, tabiat etc.

ABSTRACT

Our life span is genetically programmed and it is possible that a defect in produced proteins encoded by the ‘longevity’ gene is a cause of aging. Progeria which is a rare, fatal genetic condition which affects between one in four million and one in eight million children of both sexes equally and characterized by premature and accelerated aging. The appearance and physiology of these children resembles to elderly people but they typically have life span to their mid teens. It is also known as the Hutchinson-Gilford syndrome, which was initially reported by Johnathan Hutchinson in 1886 and further described by Hastings Gilford in 1904. It is an autosomal recessive disorder, which means an individual has inherited a mutated gene from both parents. It is added to the expanding catalogue of ‘laminopathies’, diseases caused by mutations affecting nuclear lamina proteins known as lamin A (LMNA). Currently, there are about 50 known cases of Progeria in the world and most Progeria patients die at around 13 years of age. Treatment usually includes aspirin which helps prevent the atherothrombotic events, stroke and heart attacks by hindering platelet aggregation. Vitamin supplementation, Fluoride supplements are recommended. A Study of Zoledronic acid, Pravastatin, and Lonafarnib for Patients with Progeria is ongoing, it is under phase II.

Keywords: Progeria, Hutchinson Gilford Progeria Syndrome, Premature Aging, Aspirin, Atherothrombotic, lamin A.

ABSTRACT

Triazines are interesting class of heterocyclic compounds. Various synthetic analogs of symmetric triazines have been prepared and evaluated for many pharmacological activities in different models with desired findings. Some analogs have shown potent pharmacological activity and may be considered as lead molecule for the development of future drugs. This review is an attempt to organize the chemical aspects of 1,3,5 triazine analogs reported till date systematically

Keywords:  Substituted 1, 3, 5-triazines,chemical aspects, pharmacological activities.

ABSTRACT

The present study was to evaluate preliminary photochemical analysis and in vitro antioxidant activities of leaves, fruit and stem extracts of Croton macrostachyus Hochst. (Family: Euphorbiaceae) by using different solvents like bdenzene, methanol, carbon tetra chloride and hexane. Phytochemical analysis showed the presence of alkaloids, aminoacids and proteins, flavonoids, saponins, steroids, tannins and triterpenoids. The leaves and fruits extracts were further investigated for its potential antioxidant activity by using readical scavenging DPPH (2, 2-Diphenyl-2-picryl-hydrazyl) technique. Reducing power of C. macrostachyus extracts were also screened and ascorbic acid was used as standard. Methanol extract of leaves and benzene and methanol extracts of fruits were exhibited a noteworthy DPPH radical scavenging activity compared to standard. The results were concluded that extracts have a more secondary metabolites and potential source of antioxidants, which is warranty to evaluate further in vivo pharmacological studies.

Keywords: Croton macrostachyus L, phytochemical analysis, in vitro Antioxidant activity, traditional medicine

ABSTRACT

A simple, sensitive and accurate method employing HPTLC has been developed and validated as per ICH guidelines for determination of Bosentan in bulk and Tablet dosage form. The absorption maxima of the drug were found to be 288 nm in methanol. The method was validated as per ICH guidelines. The linearity range was found to be 50-300 ng/ml with a regression coefficient of 0.98.Subsequent validation parameters like precision, repeatability in terms of Interday and Intraday precision and recovery studies were evaluated with satisfactory results, the % RSD for these parameters was found to be 1.73%,1.30-0.48%,1.80 – 0.45 % , 1.54 – 1.48 % respectively with an Rf value of 0.23.

Keywords: Bosentan, High Performance Thin Layer Chromatography, Validation

ABSTRACT

The Developed RP- HPLC method allows rapid and precise determinations of Cefixime  and Paracetamol. The scope of the present work is to expand and optimization of the chromatographic conditions and to develop RP-HPLC method. A series of mobile phases and columns were tried, among the various mobile phases, Buffer: Acetonitrile (65:35A) (PH-3.5) as an ideal mobile phase, since it gave a good resolution and peak shapes with perfect optimization. The flow rate was optimized at 1 ml/min. The Linearity and correlation coefficient of Cefixime and Paracetamol was found to be 0.999, and 0.999 respectively. Precision was performed and % RSD for Cefixime and Paracetamol were found to be 1.17% and 1.32% respectively. Three concentrations 50%, 100%, 150%, were injected in a triplicate manner and amount recovered and % Recovery was found to be 100%. Limit of detection was calculated by standard deviation method Cefixime and Paracetamol and LOD for Cefixime and Paracetamol were found to be 0.03and 0.02 respectively. Limit of Quantification was calculated by standard deviation method Cefixime and Paracetamol and LOQ for Cefixime and Paracetamol were found to be 0.08 and 0.06 respectively. Small deliberate changes in method like flow rate, mobile phase ratio, and temperature are made but there were no recognized change in the result and are within range as per ICH Guide lines. The average % Assay was calculated and found to be 100.46% and 99.84% for Cefixime and Paracetamol respectively. Hence, the chromatographic method developed for Cefixime and paracetamol is said to be rapid, simple, specific, sensitive, precise, accurate and reliable that can be effectively applied for routine analysis in research institutions, quality control department in Industries, approved testing laboratories, Bio-pharmaceutics and Bio-equivalence studies and in clinical pharmacokinetic studies.

Keywords: Cefixime, Paracetamol, Optimization, RP-HPLC.

ABSTRACT

The present work deals with the formulation and evaluation of floating tablets of Pregabalin using Thermoplastic granulation or Melt granulation technology¹. Thermoplastic granulation is a process by which granules are obtained through the addition of a meltable binder which melts during the process. This technology is used to modify or control drug release of highly water soluble drugs using hydrophobic meltable binders as done in this present work. Pregabalin is a primary medication for epilepsy, neuropathic pain, and fibromyalgia was selected for this work. The primary objective was to formulate and evaluate floating tablets of the Pregabalin by using different meltable binders like stearic acid, bees wax, carnauba wax along with other excipients such as HPMC K4M (3000cps), ethyl cellulose, sodium bicarbonate in various proportions by employing thermoplastic granulation method Pregabalin has absorption window in the upper region of small intestine hence it is suitable candidate for floating systems. FTIR spectroscopic studies suggested that the drug is compatible with all excipients used in this formulation. The formulations were evaluated for the pre-compressional and post-compressional parameters. The floating tablets were evaluated for the floating ability and also percentage drug release by using 0.1 N HCl as dissolution medium. The formulation F10 with stearic acid as the meltable binder along with ethyl cellulose had floating ability of not less than 12 hours with a good drug release profile. The optimized formulation followed Higuchi mechanism which shows both diffusion and erosion.

Keywords: Pregabalin, Stearic acid, bees wax, carnauba wax, sodium bicarbonate and HPMC K4M (3000cps).

ABSTRACT

The purpose of the research was to prepare and evaluate Roxatidine acetate HCl floating microspheres by ionotropic gelation method. Fourteen formulations were prepared, among all the formulations F13 was selected as optimized formulation based on the micromeretic and evaluation parameters including drug release studies. In the in vitro release study of formulation, F13 showed 95.65% drug release after 12 h in a controlled manner, which is desired for disease like peptic ulcer. In vitro release profiles from optimized formulation F13 were applied on various kinetic models. The best fit with the highest correlation coefficient was observed in zero order and Higuchi model, indicating diffusion controlled principle. The innovator Rotane 150 mg conventional tablet showed the drug release of 96.45% within 1 h. FT-IR and DSC analyses confirmed the absence of drug-polymer interaction. The results obtained from evaluation and performance study of different types of Roxatidine microspheres showed that system may be useful to achieve a controlled drug release profile, reduce the dose of drug, dosing frequency and improve patient compliance when compared with marketed product.

Key words: Roxatidine, buoyancy, HPMC, gum olibanum, microspheres.

ABSTRACT

In the present research work mucoadhesive microspheres of Cimetidine were prepared using Ionotropic gelation technique. All the microspheres were characterized for particle size, scanning electron microscopy, FT-IR study, DSC, percentage yield, drug entrapment, stability studies and for in vitro release kinetics and found to be within the limits. Among all the formulations M12 was selected as optimized formulation based on the physicochemical and release studies. In vitro drug release study of optimized formulation M12 showed 99.12% after 12 h in a controlled manner, which is essential for anti ulcer therapy. The innovator Cimetine conventional tablet showed the drug release of 96.15% within 1 h. The drug release of Cimetidine optimized formulation M12 followed zero order and Higuchi kinetics indicating diffusion controlled drug release.

Keywords: Cimetidine, mucoadhesion, chitosan, gum kondagogu, xanthan gum.

ABSTRACT

Overweight and obesity is one of the major health hazard, an epidemic of 21^st century and increasing worldwide. Women tend to gain weight with progression of age. The present study aimed to compute changes in obesity related health risk like weight, body mass index (BMI), waist circumference (WC), waist hip ratio (WHR), visceral fat (VF) and percent body fat (PBF), physical activity level (PAL) and dietary intake in different age groups of  obese working women  in B.H.U (respondents). For this cross – sectional study was done on 200 respondents and they were selected by purposive sampling technique. Pre-tested and pre-designed questionnaire-cum interview schedule was used for data collection. Anthropometric measurements were taken by standard technique (Jelliffe, 1966). The values of PBF and VF were taken by Omron Body Composition Monitor, HBF 212. The relationship between obesity related health risk, PAL and dietary intake was determined in three age groups i.e. ≤ 35 years, 36 - 50 years and > 50 years. A gradual increase in obesity health risk i.e. height, weight, BMI and PBF was observed with the advancement of age but it is not so in case of WC, WHR and VF. The PAL value ranges between 1.40 – 1.99 and the mean physical activity score was 1.58 ± 0.11. The PAL values showed that majority of respondent’s falls in the category of sedentary lifestyle. The protein, carbohydrate, calcium, phosphorus and total fibre intake was higher in all the age group as recommended by recommended dietary allowances (RDA), 2010. Correlation between ages, obesity related health risk and nutrient intake was observed from the value of Pearson Correlation Coefficient (r).The age shows correlation with weight (r= 0.195, P < 0.01), BMI (r= 0.190, P < 0.01), WC (r= 0.74, P < 0.05) and PBF(r= 0.472, P < 0.001) and a negative correlation with calcium (r= - 0.178, P <0.05). Therefore a diet with adequate amount of nutrients as recommended by RDA 2010 combined with exercise has a potential to substantially reduce the burden of overweight and obesity.

KEYWORDS: overweight, obesity, age, physical activity level, sedentary, dietary intake

ABSTRACT

The use of bronchodilators has been increasing for the past few decades. Study was planned to evaluate the rational use of bronchodilator drugs by analyzing the appropriateness of the prescription. A prospective observational study was conducted in all the patients who were prescribed with bronchodilators in the pediatric ward. The demographic data and the bronchodilator prescribed were recorded in the data entry format. In the study population of 133 wheezing associated with lower respiratory tract infection was the most predominant disorder found in 35.3% children.  Of the 133 pediatric patients, the major prescription was for SABA (Short Acting Bronchodilators) (99.2%). Of which the major prescription was for salbutamol (63.2%). Most of the children with asthma were prescribed with combination therapy of salbutamol and ipratropium (81.3%). In WALRI (Wheezing Associated Lower Respiratory Tract Infection), patient were prescribed with salbutamol (40.4%) and. In acute bronchiolitis, the major prescription was found to be salbutamol and ipratropium combination (70.3%). In 52.6% of the prescriptions bronchodilator were given by nebulization and oral route, 31.6% were given by nebulization. In 95.5% of patient antibiotics were prescribed along with bronchodilators, followed by mucolytic 55.6% .Other concurrent prescriptions were with steroids (38.3%). It was found that 77.4% of pediatric patients not received any oxygen supplementation. The study found over use of antibiotics, sedatives and mucolytics and under use of steroids. Bronchodilator use was optimal but evaluation of therapy was not done commonly. The study highlighted the need for a local protocol and continuing staff and parent education.

Keywords: Asthma, Bronchodilators, Salbutamol, SABA, WALRI.

ABSTRACT

Ulcer is lesion on skin or internal linings of organs or Gastro-intestinal tract, which leads to degradation of cells in the area of occurrence which may be followed by bleeding or cancer at later stages. Peptic Ulcer Disease known as Ulcus pepticum have mucosal erosions equal to or greater than 0.5 cm of an area of the gastrointestinal tract that is usually acidic and thus extremely painful. The present study was to evaluate Anti-ulcer activity in Trichosanthes dioica (Roxb.) via experimental ulcer models in animals through Histopathology study of Rat’s stomach. The leaves of Trichosanthes dioica (Roxb.) were collected from farms in and around Hastinapur district. Around two kilograms of the leaves of plant shrub were collected and were kept in shade for the purpose of drying the leaves completely. Sprague-Dawley rats (150 – 200 g) were procured from the animal house of Subharti University (n=90). The three animal models were used for the present study, mainly, Pylorus ligation, Ethanol Induced and Indomethacin (NSAID’s) ulcer models. Five groups of Animals were made, with n=6 for each group. The histopathology study of rat’s stomach was carried out for each ulcer model, and during the examination of rat’s stomach, it was clearly shown, that Trichosanthes dioica has potent Anti-ulcer activity. The Research thus primarily focuses using the plant for further study and to bring an effective and efficient ulcer healing drug in the market.

Keywords: Trichosanthes dioica (Roxb.), Methanolic extract of Trichosanthes dioica (MeTD), Anti-ulcer activity, Histopathology study

ABSTRACT

The aim of present investigation was to develop a simple UV-visible spectrophotometric method for the determination of Ibuprofen (IBF) in its pure form and marketed formulations and to validate the developed method. Ibuprofen was estimated at UV maxima of 222.8 nm in pH 7.2 phosphate buffer using UV-Visible double beam spectrophotometer. Following the guidelines of International Conference on Harmonization (ICH), the analytical parameters like linearity, precision, and accuracy were studied. The obtained results of analysis were validated statistically and by performing recovery studies to confirm the accuracy of the proposed method. In the developed method, linearity over the concentration range of 2-20 µg/ml of IBF was observed and was found in agreement of Beer’s law. The linear regression was found to be 0.999. The precision (intra-day & inter-day) of method was found within limits (RSD < 2%). The sensitivity of the method was assessed by determining limit of detection and limit of quantification. It could be concluded from the results obtained that the method for estimation of IBF in pure form and in marketed tablets is simple, rapid, accurate, precise and economical and can be used, successfully, in the quality control of pharmaceutical formulations and routine laboratory analysis.

Keywords: Ibuprofen, UV Spectrophotometer, Inflammation, Validation.

ABSTRACT

This study aims to study the diversity of bacteria in different water samples which taken from Meet Faris drinking water station, during the period from July, 2013 till June, 2014. The bacteriological analyses involved total bacterial counts (TBCs), total coliforms (TC) and estimation of fecal coliforms (FC), fecal streptococci and pathogenic bacteria. Fifty pathogenic bacterial isolates obtained from raw water samples. The most prevalent organisms were E.coli (30%), Klebsiella.spp (14%), Pseudomonasspp(16%), Proteus. Spp (10%), E. fecalis (14%) Shigellaspp.(8%), Staph.coccus (8%). According to antibiotic susceptibility test results, enrofloxacin and gentamicin were the most effective antibiotic on E.coli isolates. The obtained results revealed that, the River Nile water was subjected to sewage pollution. Detection of E.coli by PCR was found to be important for confirmation of the detected E.coli isolates.

Keywords: Pathogenic bacteria, Antibiotic test, PCR, Meet Faris, River Nile

ABSTRACT

Dalbergia sissoo (family: Fabaceae) is an Asian deciduous rosewood tree. It is the state tree of Punjab state (India) called as Shisham used for antipyretic, emesis, ulcers, leucoderma, stomach troubles and skin disease, memory enhancer etc. The aim of this study is to evaluate the antidepressant activity of ethanolic leaf extracts of Dalbergia sissoo in mice. The animals were divided into five groups of 6 each. Group I was considered as normal control, II as Standard control (Imipramine), III, IV and V was treated group (ethanolic leaf extracts of Dalbergia sissoo 300, 450 and 600 mg/kg respectively). The animals were acclimatized for behavioral tests like Tail suspension test and Forced swim Test. In behavioral model of depression Tail suspension test and Forced swim Test, ethanolic leaf extracts of Dalbergia sissoo decreased the immobility time significantly and increase in the first latency in dose dependent manner. The findings in the behavioral model of depression showed significant effect was due to the monoamine theory of depression.

Keywords: Dalbergia sissoo, ethanolic leaf extracts of Dalbergia sissoo, Tail suspension test, Forced swim Test, Imipranine.

ABSTRACT

Gemifloxacin mesylate loaded microspheres were prepared by Ionotropic gelation technique with different drug to carrier ratio. All the microspheres were characterized for particle size, scanning electron microscopy, FTIR study, DSC, percentage yield, drug entrapment, stability studies and for in vitro release kinetics and found to be within the limits. Among all the formulations S8, was selected as optimized formulation based on the physic chemical and release studies. In the in vitro release study of formulation S8 showed 95.92%, after 12 h in a controlled manner, which is essential for anti ulcer therapy. The innovator Gemiflox conventional tablet shows the drug release of 95.23% within 1 h. The drug release of optimized formulation S8 followed zero order and Higuchi kinetics indicating diffusion controlled drug release.

Keywords: Gemifloxacin mesylate, gelatin, microspheres, scanning electron microscopy, release order kinetics.

ABSTRACT

Present study aims to prepare and evaluate mucoadhesive microspheres by ionotropic gelation method. Among all the formulations M10 was selected as optimized formulation for mucoadhesive microspheres based on the evaluation parameters and drug release studies. In vitro release study of formulation M10 showed 97.11% 12 h in a controlled manner, which is essential for disease like peptic ulcer. The release order kinetics for M10 was best fit with the highest correlation coefficient was observed in Higuchi model, indicating diffusion controlled principle. The innovator Abygate conventional tablet shows the drug release of 97.23% within 1 h. FT-IR and DSC analyses confirmed the absence of drug-polymer interaction. The results obtained from evaluation and performance study of Gatifloxacin mucoadhesive microspheres that system may be useful to achieve a controlled drug release profile suitable for peroral administration and may help to reduce the dose of drug, dosing frequency and improve patient compliance when compared with marketed product.

Keywords: Gatifloxacin, mucoadhesiveness, gum olibanum, chitosan, microspheres.

ABSTRACT

The aim of the present work was to develop and optimize gastroretentive floating system of Gemifloxacin mesylate using HPMC polymers, Gelucire 50/13 and Polyox WSR 301 to improve oral bioavailability of Gemifloxacin mesylate floating tablets by increasing gastric residence time. The tablets were prepared by direct compression method. The effect of polymers concentration and viscosity grades of HPMC on drug release profile was evaluated. The result of in vitro dissolution study showed that the drug release profile could be sustained by increasing the concentration of HPMC and Polyox WSR 301. The optimized formulation (F12) containing HPMC K100M, Gelucire 50/13 and Polyox WSR301 showed 99.12% drug release at the end of 12h. The optimized formulations (F12) containing showed desired buoyancy (floating lag time of about 35 seconds and total floating time of >12h). Optimized formulation (F12) followed diffusion controlled zero order kinetics and non-fickian transport of the drug. FTIR studies revealed the absence of any chemical interaction between drug and polymers used.

Keywords: Gemifloxacin mesylate, floating drug delivery system, HPMC, WSR 301, floating lag time

ABSTRACT

Two sensitive and reproducible methods are described for the quantitative determination of Glipizide and Metformin Hydrochloride in presence of its degradation products. The first method was based on high performance liquid chromatographic (LC) separation of the drug from its degradation products on the reversed phase, Cosmosil^® column [C₁₈ (5 mm, 4.6 x 150 mm, i.d.)] at ambient temperature using a buffer consisting of 10 mM potassium dihydrogen phosphate (pH adjusted to 2.5 with diluted o- phosphoric acid) and acetonitrile 50: 50 v/v as optimized mobile phase in a gradient program. The flow rate was 0.7 ml min^-1 and quantitation was achieved UV determination at 225 nm based on peak area with linear calibration curves at concentration range 10-25 µg ml^-1 and 20-50 µg ml^-1 respectively. The second method was based on   high performance thin-layer chromatographic (HPTLC) separation followed by densitometric measurement of spots at 216 nm. The separation were carried out on Merck HPTLC aluminium sheets of silica gel 60 F ₂₅₄ using Toluene: Methanol: Ethyl acetate: Formic acid in the ratio of (3:6:3:0.2, v/v/v/v), as mobile phase. This system was found to give compact spots for Glipizide and Metformin hydrochloride after double development (retention factor, R_F 0.08 ± 0.02 and R_F 0.74 ± 0.02 respectively). The second order polynomial regression analysis data was used forth regression line in the range of 200-1400 ng spot^-1 and 200-1400 ng spot^-1 respectively. Both the method has been successively applied to pharmaceutical formulation. No chromatographic interference from the tablet exicipients was found. Both the methods were validated in terms of precision, robustness, recovery, limits of detection and quantitation.

Keywords: Glipizide, Metformin Hydrochloride, reverse phase high performance liquid chromatography, high performance thin-layer chromatography, Quantitative Analysis, Validation, stability indicating procedure, pharmaceutical formulation.

ABSTRACT

The objective of the study was preparation of sustained release matrix tablets by hot melt extrusion (HME) and process optimization for continuous manufacturing. Furthermore, HME tablets were evaluated with respect to in vitro release rate, erosion behavior and water uptake study. Hydroxypropylcellulose (HPC) was used as release retarding polymer. The drug chosen for study was first line anti tuberculosis drug rifampicin. 50 % drug loaded HME tablets were prepared. The HME tablets were characterized by DSC, FTIR and SEM. No chemical interaction was found between drug and polymer as per DSC and FTIR. Dispersion of drug particles and internal micro pores was observed by SEM. In vitro release study revealed 50% drug loaded HPC matrix tablets gave sustained release of 101.41±1.02% at the end of 24 h. Release rate of rifampicin from HME tablets was found to be dependent on the concentration of polymers and plasticizer. The release rate from the edges and circumference of tablets suggested the hydration of the tablets from the circumference was more significant than at edges of the tablets. Drug release from HME matrix tablets was found to follow Super case-II transport mechanism. HME tablets were stable for six months as per ICH guideline.

Keywords: Hot Melt Extrusion (HME), Hydroxypropylcellulose (HPC), Rifampicin, Sustained release, Korsmeyer–Peppas model

ABSTRACT

Accelerated stability studies of Emblica officinalis, Terminalia belerica and Terminalia chebula have been carried out as per ICH guidelines and its effect on total polyphenol content as determined by Folin-Ciocalteu method and Gallic acid content as determined by HPLC (High Performance Liquid Chromatography) was studied. The samples were kept in stability chamber at 40°C and 75% relative humidity for 3 months for accelerated stability studies. Samples were taken out at periodic intervals and extracted to determine total polyphenol content by spectrophotometric method and gallic acid content by HPLC. The HPLC method was also validated to demonstrate its selectivity, linearity, precision, and accuracy. The results indicate an increase in total polyphenolic content as well gallic acid content under accelerated stability conditions which is indicative of hydrolysis of gallotannic acids present in crude drugs to liberate free gallic acid, thereby increasing the total polyphenolic content.

Keywords: HPLC; polyphenols; gallic acid; Emblica officinalis; Terminalia belerica; Terminalia chebula

ABSTRACT

This study investigates the stability of paracetamol pediatric oral suspension (120mg/5ml) in simulated in-home storage conditions at temperature ranging from (2-8C⁰) representing refrigerator condition. Samples from suspension were assayed and tested for related substance (degradants) using B.P pharmacopeia HPLC method. The study was performed in day zero, seven, fourteen, thirty and forty five.  The instrument employs column ® C8, 100 x 4.6 mm, 3.5 μm particle size. The mobile phase consisted of methanol, tetrabutylammonium hydroxide (40 %) and sodium orthophosphate buffer. The results showed that the drug assay content remains within the limits up to day fourteen. Furthermore, the half live was found to be 36.8 days.

Keywords: Paracetamol, 4-amino phenol, degradation, HPLC

ABSTRACT

A simple, precise and stability-indicating HPLC method was developed and validated for the simultaneous estimation of anti-retroviral drugs Lopinavir and Ritonavir. The separation was achieved on AgilentC8, 150mm* 4.6 ,5µ  column with isocratic flow. The mobile phase at a flow rate of 1.5ml consisted of 0.05M Potassium Dihydrogen Orthophosphate buffer and Acetonitrile: MeOH in the ratio of (80:20).The ratio of buffer: organic is (45:55).The UV detection was carried  out at 210nm. The method was successfully validated in accordance to ICH guidelines. This method was then used to study the stability aspects of both the drugs when subjected to acidic, alkaline, thermal and photo degradation condition.

Keywords: Lopinavir, Ritonavir, Stability Indicating Assay Method, RP-HPLC.

ABSTRACT

In the present study N-(2-oxosubstitutedindolin-3-ylidine)-2-phenylacetohydrazides (IV a-h) have been synthesized in good yields and characterized by IR, PMR and mass spectral analyses. Compounds were evaluated for their preliminary in vitro cytotoxic activity against HeLa cancer cell lines by standard MTT assay and also were screened for antioxidant activity by DPPH method. Our results shown that two of the analogues IVf and IVc  are potent antioxidant agents and IVb and IVg are potent cytotoxic agents.

Keywords: Isatin, antioxidant, cytotoxic.

ABSTRACT

Indomethacin is a drug belongs to class NSAIDs used in the treatment of inflammatory rheumatoid diseases and relieve acute pain, period pain and pain after surgery and fever. This study aimed at evaluating some quality control parameters to compare the quality, safety, and efficacy of three brands of Indomethacin capsules available in the Indian market. In the present study three marketed formulations of Indomethacin of 25 mg strength were analyzed with quality parameters like Weight variation test, Disintegration test and In-vitro bioequivalence study with developed spectrophotometric analytical method. The Indomethacin capsule, Microcid exhibited highest in-vitro drug release 97.05% and lowest Disintegration time 320 sec. compared to other brands of Indomethacin capsule.  

Keywords: Indomethacin, In-vitro release study, Spectrophotometric analysis method development, Bioequivalence.

ABSTRACT

The study was undertaken with an aim to improve the efficacy and reduce the adverse effect of drug, by combination therapy of  Diltiazem HCL and Quercetin dihydrate. In the present research 22 formulations were developed using design expert software with response surface methodology. In which the effect of superdisintegrant, type of superdisintegrant, effect of diluents, formation of solid dispersion studied for their in vitro release  from pellets. The result depicted that the formulation containing superdisintegrant crospovidone, diluent lactose and presence of surfactant  showed good disintegration time and in vitro drug release.

Key words: Diltiazem HCL, Quercetin, Pellets, Immediate release

ABSTRACT

Zidovudine (AZT) is an antiretroviral drug with activity against Human Immunodeficiency Virus (HIV) Type 1. However, only temporary and limited benefits are observed in HIV infected patients treated with zidovudine alone or in combination with other antiretroviral drugs. Upon oral administration, it exhibits dose dependent toxic effects such as hepatotoxicity, hyperglycemia, hyperlipidemia, lactic acidosis, lipodystropy, osteonecrosis. These side effects often require dosage reduction or even cessation of treatment. Hence, in the present work an attempt is being made to develop a stable drug delivery system for zidovudine in the form of controlled release microbeads incorporated with different types of waxes. Wax incorporated microbeads of Zidovudine were prepared by melt extrusion-ionotropic gellation method. A series of tests have been carried out to characterize the microbeads in vitro, including particle size distribution, SEM analysis, loading parameters, in vitro release studies and stability studies. Compatibility studies proved that there was no interaction between zidovudine and different waxes used. Zidovudine beads were roughly spherical in nature, which was confirmed by Scanning electron microscopy. Zidovudine loaded beads with normal frequency distribution were obtained. A maximum of 74.65% drug entrapment efficiency was obtained. The in-vitro performance of Zidovudine beads showed sustained release up to 24 hrs depending on the wax concentration. Finally it can be concluded that the formulated matrix type microbeads with bees wax were more feasible and effective than carnauba wax beads in encapsulating zidovudine and thereby increasing the effectiveness of the drug.

Keywords: Zidovudine (AZT), Controlled release, Alginate gel beads, Natural waxes.

ABSTRACT

To identify level of depression for sixth class of secondary  school. To identify the effect of depression learning status. To determine the reason that lead to depression. A cross sectional study was conducted from 11th December, 2014 up to 10th march, 2015 in order to study incidence of  depression among sixth class of secondary school students in al-najaf city. The study was carried out in the secondary schools ( Khaurnq, Sidrat  Almuntaha, Kufa, Najaf, Muslim Ibn Aqil, Sheikh al mufeed  , aminh al sadeer, al ameer, Lathiqia) at AL-Najaf city. a questionnaire format was designed and constructed by researchers to achieve objective the study .   the questionnaire format  consisted of two  parts  the part 1 socio demographic characters sheet consist of 4 items which include age ,gander ,parents occupation ,parents education level, residence. Part 2 include  10 items related to depression, not at all 1, several day 2 ,more than half the 3, nearly every day 4. A randomized  sample of  150  students  were collected from 10 secondary schools with range 15 students from each school. The present study found that the depression scale of more than half the days were increased and highest within the secondary sixth class students at age <= 18 years while the lowest depression scale  more than half the days highly significant differences. The depression scale within the males sample was higher than females with high significant. The study shows there was no significant difference of depression scale within other socio-demographic characteristic. The study should be conducted on large population within more duration time of interviewing to have the best and accurate results. Using a health education program within the questionnaire format during student's interview

Keywords: Incidence of, Depression, Among, Sixth Class, Secondary, School Students

ABSTRACT

Strongyloides stercoralis is a persistent pathogenic roundworm commonly known as “hidden killer”. Its ability to replicate in human host, cyclic autoinfection that can last for years and asymptomatic behavior make theranostics difficult. Ajuga integrifolia is a shrub that is traditionally claimed to possess a very potent effect against persistent gastrointestinal ailments. The objective of this study was to analytically investigate the anthelmintic activity of methanolic extract of aerial parts of A. integrifolia on rhabditiform larvae of S. stercoralis. The larvae were isolated from fresh stool samples obtained from school children diagnosed to be positive for the parasite. The anti-S. stercoralis effect of the extract (in phosphate-buffered saline (PBS): sterile, pH = 7.2, 1.7 mM) against rhabditiform larvae was evaluated by incubating the suspension of the parasites in PBS with different concentrations of the extract for 24 h at 37 ⁰C in a 5 % CO₂ humidified incubator to determine % survival. A concentration dependent killing effect with an IC₅₀ value of 50 mg/mL was recorded. The sensitivity and immediacy of action proved a potential commercial value of the plant for treatment against human strongyloidiasis.

Keywords: Strongyloides stercoralis, Ajuga integrifolia, crude extract, anthelmintic activity

ABSTRACT

A simple, precise, accurate, simultaneous and stability-indicating HPLC method developed with an effective resolution of active pharmaceutical ingredients. The present method effectively separates all the related substances of Diphenhydramine hydrochloride and acetaminophen along with impurities. Chromatographic separation has been obtained on Inertsil C18 (250 X 4.6mm, 5µ) column using a gradient elution with a mixture of phosphate buffer pH3.0 and acetonitrile. At 220 nm compounds will be eluted and monitored. Diphenhydramine hydrochloride and acetaminophen were subjected to the stress conditions of acid, base, peroxide, thermal, photolytic, humidity and water degradation. The degradation products were well resolved from main peak and its impurities, proving the stability-indicating ability of the method. The developed method was validated as per International Conference on Harmonization (ICH) guidelines and validation acceptance criteria were met in all cases. The current method has proven good linearity and accuracy over the range of all known impurities from LOQ to 150% of the target concentration. The degree of reproducibility, as results obtained by deliberate changes in the method parameter and variety of condition has proven that the method is robust and rugged.

Keywords: HPLC, Stability indicating, Acetaminophen, Diphenhydramine Hydrochloride, Related substances. 

ABSTRACT

A stability-indicating HPLC method was developed and validated for the quantitative determination of diacerein in capsule dosage form. An isocratic separation was achieved using a C18, 250×4.6 mm, 5 µm particle size column with a flow rate of 1 ml/min and using a UV detector to monitor the eluent at 258 nm. The mobile phase consisted of Water: acetonitrile (70:30v/v). The drug was subjected to oxidation, hydrolysis, neutral, thermal and photolytic degradation. Diacerein was found to degrade under acidic, basic, oxidative, neutral and also dry heat condition. Complete separation of degraded products was achieved from the parent compound. All degradation products were eluted in an overall analytical run time of approximately 10 min with the parent compound diacerein eluting at approximately 6.44 min. The method was linear over the concentration range of 5-15 µg/ml (R² = 0.999) with a limit of detection and quantitation of 0.0093 and 0.028 µg/ml respectively. The method has the requisite accuracy, selectivity, sensitivity, precision and can be used to assay diacerein in tablet. Degradation products resulting from the stress studies did not interfere with the detection of diacerein and the assay is thus stability-indicating.

Keywords: Diacerein, Degradation, HPLC-UV.

ABSTRACT

The present work describes the formulation development of mouth dissolving tablets of Promethazine HCl with an optimum dispersion time along with sufficient hardness. The formulation employed three different super disintegrants, namely crospovidone (CP), sodium starch glycolate (SSG) and crosscarmellose sodium (CCS), each in three different ratios. Microcrystalline cellulose and mannitol were used as binder and diluent respectively. FT-IR and DSC were used to study the drug-excipient compatibility. Preformulation studies were carried out so as to study the compression characteristics and the flow properties of the powder mix, which was within satisfactory limits. Formulations were made by direct compression method and evaluated for in vitro dispersion time (DT), hardness, friability, wetting time, and in vitro dissolution rate. The effect of DCP and lactose as a diluent was evaluated. All the formulations showed a DT below 4 min. with hardness of 2.9 kg.cm^-2 or above. Tablets containing CP at 10%W/W with a hardness of 3.25 kg.cm^-2 and DT of 17 S was chosen as the most satisfactory formulation which released the complete drug in 4 min. The other super disintegrants yield tablets of nearly lesser hardness (upto 2.9 kg.cm^-2) with higher DT (upto 216 S). DCP and lactose increased the DT without major effect hardness of tablets.

Keywords: Mouth dissolving tablets, super disintegrants, promethazine hydrochloride, in vitro dispersion time, wetting time.

ABSTRACT

In the present study, various extracts of Nardostachys jatamansi roots were tested against the head louse Pediculus humanus capitis. Chloroform, petroleum ether, methanol, and water extracts of N. jatamansi roots were used for determining Potential pediculocidal and ovicidal activity using filter paper diffusion method. It was observed that methanol extracts exhibited excellent anti-lice activity with values ranging between 50.3% and 100% where as peteroleum ether, chloroform and water extracts showed moderate pediculocidal effects. All the results were well comparable with benzoyl benzoate (25% w/v) was used as positive control to compare the activity. Anti-lice activity of N. jatamansi extracts proved a potential prospect of introducing it in anti-lice formulations.

Keywords: Nardostachys jatamansi, roots, anti-lice activity, filter paper bioassay, head louse, paper diffusion method, ovicidal activity

ABSTRACT

Valacyclovir hydrochloride  is widely used for the treatment on Herpes virus, illness caused by Herpes virus such as Genital herpes, Cold sores, Chingles and Chicken pox. The present study is deals with formulation, optimization, evaluation of Valcyclovir HCL mouth dissolving films. Genital herpes, Cold sores, Chingles and Chicken pox are the conditions where instance effect of drug is required. Valacyclovir hydrochloride is one of the drug which is used in the treatment of above three disease conditions. The mouth dissolving films was prepared by using solvent casting method. The concentration of propylene glycol, sodium lauryl sulphate (SLS) were kept constant in all formulations (F1-F4) and varying concentration of hydroxy propyl methyl cellulose(HPMC) and methyl cellulose. All the formulations were evaluated for surface pH, weight uniformity, folding endurance, drug content, disintegration time, in-vitro dissolution studies. The formulation ‘F3’ was found to be optimized formulation. It shows results for all evaluation parameters such as weight variation 34.70±0.7mg, surface pH 6.75±0.60, folding endurance > 100, drug content 95.25±1.10%, disintegration time 30±0.50 sec, and in-vitro dissolution study 81.35±1.30 % at the end of 5 min.

keywords: Fast dissolving film, Valacyclovir hydrochloride, Solvent casting, Hydroxyl propyl methyl cellulose, Chicken pox, Genital herpes.

ABSTRACT

A. Racemosus; Aqueous Extract; Paw volume; Erythrocyte sedimentation rate (ESR). Asparagus Racemosus (Linn) popularly called as Challan gadda belongs to Asparagaceae family. Phytochemical constituents such as Steroidal saponins, glycosides, Oligospirostanoside, Isoflavones, Furan compounds and Flavonoids have been reported in  A. Racemosus. In the present study the roots of Asparagus Racemosus were studied for anti arthritic activity The antiarthritis activity was evaluated by using FCA induced arthritis model in Wistar rats. The assessment made during 32 days showed that. The parameters evaluated in this study are Body weight, Paw volume, White blood cell count (WBC),Red blood cell count (RBC),Hemoglobin count (Hb), Erythrocyte sedimentation rate (ESR). The statistical data indicated that the Aqueous Extract of Asparagus racemosus root (200mg/kg) and (400mg/kg) was administered 1 hr before the administration of Freund’s Complete - Adjuvant (0.1ml. subplanetar region). ***P <0.05 and ***P <0.005 significant compared to control group respectively. The experimental data demonstrated that A. Racemosus displayed remarkable antiarthritic activity.

Keywords: Antiarthritic activity, Aqueous Extract, A. Racemosus

ABSTRACT

Candesartan cilexetil is an antihypertensive drug effective for the treatment of hypertension and heart failure. The main goal is to formulate and evaluate the sustained release matrix tablets of candesartan cilexetil using different polymers like hydrophilic and hydrophobic. Different formulations were prepared by direct compression method using various release retarding polymers like carbopol 934P, HPMC K15M, sod.CMC. Water soluble surfactant SLS was employed for enhancing the solubility of candesartan cilexetil. Drug-excipients compatibility was carried out by FTIR. Different formulations were evaluated for hardness, thickness, friability, drug content and in vitro drug release. The results were found to be satisfactory in terms of physico-chemical parameters. The F10 formulation was found to display highest drug release of drug. Mathematical analysis of the release kinetics was carried out to determine the mechanism of drug release. In vitro release data was fitted into various models to ascertain the kinetic of drug release.

Keywords: Sustained release matrix tablets, HPMCK 15M, carbopol 934P, sodium CMC, SLS, Direct compression, Candesartan cilexetil.

ABSTRACT

Cancer is the second leading cause of death globally. Cassia fistula (CF), a member of Leguminosae family, is Native to India, Amazon and Sri Lanka, is widely used for its medicinal properties in Indian system of medicine for various ailment from the ancient time. The present investigation was undertaken to investigate the anticarcinogenic action of Cassia fistula L.  extract on 2-stage skin carcinogenesis model in Swiss albino mice. The papilloma were produced on mice skin by DMBA and promoted by croton oil and one weeks later, promoted by repeated application of croton oil (1% in acetone/twice in a week) till the end of the experiment (16 weeks). After 16 weeks at the time of termination of the experiment estimation of GSH from the liver and blood tissue of the animals were also done by the method of Beutler et. al. (1963). the outcomes of the papilloma study and GSH estimation was correlated and it was found to be preventive for the formation as well as persistence of papilloma. 21 no. of papilloma were found in CF treated mice as compared to (35) untreated control mice. Our results suggest that Cassia fistula can be a cost effective future herbal alternative medicine for cancer treatment.

 Keywords: Cassia fistula, Leguminosae, Papilloma, Carcinogenesis, DMBA, Croton oil, Chemoprevention.

ABSTRACT

This study was designed to assess the blood electrolytes (Sodium, potassium, chloride, calcium and phosphate) levels in some hypertensive patients and healthy volunteers and to compare between them. The study aimed to determine possible changes in electrolyte levels of hypertensive patients in University of Port Harcourt Teaching Hospital. The study population was a randomly selected total of 120 healthy staff and student adults between 18-50 years of the University community and 120 patients of the University teaching hospital. 5mls of blood sample were collected separately from ante cubital vein of each of the study subjects. The serum electrolytes determined were sodium, potassium and chloride (Ion Selective Electrode method); calcium (Randox method) and phosphorus (Phosphomolybdate method).  Measurements of results were analyzed using statistical package for social science (SPSS) version 17.0. The mean values of potassium and chloride in hypertensive female patients were lower compared to those of control, while sodium and calcium showed no significant difference. The male category showed significant lower values in sodium, chloride and calcium while Phosphorous were higher in the hypertensive patients in both categories when compared to the healthy volunteers (control). The results obtained showed a significant difference at p < 0.05 significant level between hypertensive and healthy individuals for various blood electrolytes in both female male categories. We can then conclude that hypertensive patients and healthy individuals blood electrolytes is significantly different.

Keywords: Phosphomolybdate method, hypertensive female patients, blood electrolytes

ABSTRACT

Present study aims to prepare and evaluate mucoadhesive microspheres by ionotropic gelation method. Among all the formulations M10 was selected as optimized formulation for mucoadhesive microspheres based on the evaluation parameters and drug release studies. In vitro release study of formulation M10 showed 97.11% 12 h in a controlled manner, which is essential for disease like peptic ulcer. The release order kinetics for M10 was best fit with the highest correlation coefficient was observed in Higuchi model, indicating diffusion controlled principle. The innovator Abygate conventional tablet shows the drug release of 97.23% within 1 h. FT-IR and DSC analyses confirmed the absence of drug-polymer interaction. The results obtained from evaluation and performance study of Gatifloxacin mucoadhesive microspheres that system may be useful to achieve a controlled drug release profile suitable for peroral administration and may help to reduce the dose of drug, dosing frequency and improve patient compliance when compared with marketed product.

Keywords: Gatifloxacin, Mucoadhesiveness, Gum Olibanum, Chitosan, Microspheres.

ABSTRACT

A stability indicating reverse phase High performance liquid chromatography (RP-HPLC) method has been developed and subsequently validated for the simultaneous determination of Atazanavir and Cobicistat in bulk and pharmaceutical formulation. Separation was achieved in isocratic mode with a Kinetex C₁₈ 100 A (250 mm x 4.6 mm,  5µ) column and mixture consisting of 0.1% OPA(pH 3) and methanol in 80:20 v/v was used as mobile phase with a flow rate of 1 ml/min, column temperature at 25°C and the run time as 10 mins. UV detection was performed at 239 nm and the sample temperature was maintained ambient. The described method for simultaneous determination of Atazanavir and Cobicistat is linear over a range of 8 μg/ml to 120 μg/ml and 5 μg/ml to 60 μg/ml respectively. The method shows good precision results which were below 2.0%RSD. Limit of Detection (LOD) and Limit of Quantification (LOQ) of Atazanavir and Cobicistat was established and found to be 1.49 and 4.97 μg/ml and 1.13 and 3.77 μg/ ml respectively. The developed method was validated according to ICH guidelines for various parameters.The method is simple, rapid, selective and stability indicating method which would be used for regular stability indicating quality control determinations.

Keywords: RP-HPLC; Simultaneous Determination; Atazanavir and cobicistat; stability indicating.

ABSTRACT

A high throughput, sensitive, selective, and rugged liquid chromatography coupled with mass spectrometry (LC-MS/MS) method for the quantification of Zidovudine, Lamivudine and Nevirapine, in human plasma was developed and validated.  The analytes were extracted from plasma by solid phase extraction technique using Waters Oasis HLB 96 well plate 30 µm (30 mg). Isocratic  elution  of  Zidovudine, Lamivudine and Nevirapine  were  achieved  in  3 min  using  ACE, C18, 4.6 X 150mm, 5µ column having a mobile phase of 0.1% formic acid: Methanol 30: 70 v/v. The flow rate was 0.7 mL/min at a column temperature of 35 ± 5°C. Electron spray ionization technique in positive mode was selected to improve the selectivity and sensitivity required for this application. The retention times of Zidovudine, Lamivudine and Nevirapine were 1.5, 1.2, and 1.7 min, respectively. The method was validated for linearity, precision, accuracy, specificity, sensitivity, matrix effect, dilution integrity, ruggedness, reinjection reproducibility, and stability. The assay produced linear calibration curves over the concentration range for Zidovudine, Lamivudine and Nevirapine in the ranges of 5 to 1500, 5 to  1500 and 10 to 3000 ng/mL respectively with correlation coefficients greater than 0.9963 using a 1/x2  weighted least square regression analysis of standard plots associated with eight-point calibration standards. The precision and mean accuracy were within the acceptable limits.

Keywords: Zidovudine, Lamivudine and Nevirapine, Solid Phase Extraction and Waters Oasis HLB 96 well plate

ABSTRACT

Infestation of the head louse caused by Pediculus humanus capitis is an important public health problem worldwide. FDA has approved Ivermectin as an antilice drug in 2012. Commercially Ivermectin is available in the form of Sklice lotion in US market. Hence, in the present work an attempt was made to formulate hair gel of Ivermectin for better patient compliance and to avoid the side effects related with other formulations. The gels of 0.5% Ivermectin were prepared using different gelling agents such as carbopol 934, hydroxypropyl methylcellulose K4M, hydroxyethyl cellulose 250 HHX. Glycerin and propylene glycol were used as a humectants having plasticizer activity. The formulations were characterized for pH, viscosity, spreadability, extrudability, drug content, in vitro drug release, antilice activity, skin irritation study and stability studies. Among the selected formulations, formulation containing 2% HEC 250 HHX and 15% propylene glycol showed better viscosity, spreadability, extrudability and In vitro drug release as compared to other formulations. It showed excellent antilice activity and no skin irritation was observed. It was found to be stable at 25^°C/60% and 40^°C/75% RH over a period of 45 days. These results suggest the feasibility of the topical gel formulation of Ivermectin for the treatment of pediculosis.

Keywords:  Pediculus humanus capitis, Ivermectin, antilice, Carbopol 934, HPMC K4M, HEC 250 HHX.

ABSTRACT

In an endeavor to boost the prophylactic action of Quercetin Dihydrate against mustard agent poisoning, mucoadhesive microspheres, were formulated. The microspheres enclosed Quercetin Dihydrate, an adhesive polymer (ethyl cellulose) and a colon specific polymer (Eutragit S100). Microspheres were devised by an oil/water emulsification solvent evaporation method. Two variables polymer concentration and plasticizer concentration for formulation were used. The mean particle sizes of the prepared microspheres were found significantly increasing with polymer concentration and decreased with increasing plasticizer concentration. The drug entrapment effectiveness increased with increasing plasticizer concentration. The Percentage mucoadhesion increases with increasing concentration of ethyl cellulose but not much affected by concentration of eudragit. Drug entrapment efficiency was found in range of 73.35±2.7 (batch R1) to 80.61±1.54 (batch F5). The entire formulations had excellent flow property. The best fit release kinetic model was found to be Higuchi for all formulations, which indicated release from matrix type formulation. The In vivo studies on male wistar rats were conducted and plasma concentration time method was employed to study the influence of quercetin by formulating it as microspheres. By Statistical Analysis through sigma plot, the semi log plot of pure drug (Quercetin) and its microspheres shows linearity which indicates that they follow linear kinetics. Formulation of microspheres produced a sustained effect on its absorption and availability and several parameters are there which concluded that the microspheres of quercetin are better choice for mustard toxicity as compared to pure drug.

Keywords: Quercetindihydrate, mustard agent poisoning, mucoadhesive microspheres, polymers concentration, plasticizer concentration.

ABSTRACT

Citrullus colocynthis Schrad., traditional Tunisian medicinal plant, showed beneficial effects against oxidative stress mediated diseases, namely its fruits and seeds which contain several compounds with biological activity. The present study reports the antioxidant and the antiproliferative properties of different seed and fruit organic extracts. Antioxidant activity was assessed by the ability to quench the free DPPH and the superoxide anion radicals and inhibit the ABTS cation. Methanol extracts presented the highest DPPH scavenging (seeds IC50 = 0.178 mg/ml; fruit IC50 = 0.223 mg/ml) and superoxide scavenging (seeds IC50 = 28.102 µg/ml; fruits IC50 = 30.793 µg/ml) activities. All extracts inhibited the ABTS radical formation. The most interesting TEAC values were registered with methanol extracts (seeds = 1.225 and fruits = 1.120). Petroleum ether seed extract showed the lower antioxidant action. Seed and fruit organic extracts were also tested for their antiproliferative activity on HT-29 human cell line. All extracts induced a concentration dependent growth inhibition. Petroleum ether seed extract exhibited the higher growth inhibition activity (IC50 = 321 µg/ml), while methanol fruit extract showed the less antiproliferative efficiency (IC50 >500 µg/ml). Data obtained indicate that seeds and fruits constitute an excellent source of effective natural antioxidants and chemopreventive agents.

Keywords: Citrullus colocynthis ; phenolic contents; antioxidant; antiproliferative.