ABSTRACT

Large number of advance drug delivery in cancer therapy. The use of current drug delivery technologies in cancer therapy requires drug delivery to cancer tissue only .Nanocarriers for drug delivery in cancer therapy plays important role nowadays. Targeted therapies are generally better than traditional chemotherapy, but they are associated with several adverse effects. Natural products have long been fertile source of cure for cancer .Gene changes in cells that cause cancer, they have been able to develop drugs that targeted these changes treatment with these drugs is called targeted therapy. Targeted therapy is used to keep cancer from growing and spreading. Nanocarrier is nanomaterial being used as transport module for another substance such as drug commonly used nanocarriers includes, micelles, polymers, carbon based material, liposome and other substances.

Keywords: CMC-Critical Micelle Concentration, RES-Reticular endothelial system, HIV-Human immunodeficiency virus, and HIFU-High intensity focused ultrasound, MABs-monoclonal antibodies, HBV-Hepatitis B.

ABSTRACT

Process analytical technology (PAT) has been defined as a mechanism to design, analyze and control pharmaceutical manufacturing processes through measurement of critical process parameters which affect critical quality attributes. PAT checks the quality of raw material attributes both physically and chemically (i.e. at off-line, on-line, in-line). PAT involves a shift from testing the quality of building to the quality of products by testing at several intermediate steps. PAT saves a huge amount of time and money required for sampling and analysis of products. Pharmaceutical companies face many challenges and problems while implementing PAT into their new and pre-existing manufacturing processes. The potential for improved operational control and compliance resulting from continuous real time quality assurance was highlighted as a likely benefit that would result from PAT implementation. In this paper, we will start with brief PAT concepts, Introduction, PAT tools, Pat implementation and a review of their application in the wider pharmaceutical industry.

Keywords: Hyphenated techniques, NMR, High performance liquid chromatography, Critical Process parameters (CPP).

ABSTRACT

Diabetes mellitus and Hypertension are a common disease that is suffered by a huge percentage of total population. The coexistence of these two diseases is at a greater frequency than alone. Hypertension in the diabetic individual potently increases the risk and accelerates the risk of cardiac disease, stroke, peripheral vascular disease, nephropathy and retinopathy. The management of both this disease is equally important and the reduction in cholesterol level have significant role in preventing diabetic complication. Diabetic associated diseases like nephropathy also lead to the development of hypertension particularly in type I diabetic patient. The coexistence of hypertension in both type I and type II diabetic patients can lead to be increased peripheral vascular resistance and the exchangeable sodium ion can be a reason for hypertension in diabetics. The insulin resistance or hyperinsulinemia or elevated insulin can be one of the major pathogenesis of hypertension. In the present study we have reviewed the various literatures related to the coexistence of to life threatening disease that is hypertension and diabetic and it was observed that these two diseases are most commonly associated in a person. Thus there should be some modified treatment procedures for this kind of life threatening associated diseases.   

Keywords: Diabetes Mellitus, Hypertension, Coexistence.

ABSTRACT

Shakhas are important part of the body as they form a part of karmendriyas and the main angas among the sakhas. In ayurved the structure sira is of vital importance, we can see elaborate description about the siras in various classical texts .There are difference in the opinion regarding siras  in different classics. Rakta mokshana is a treatment modality which covers half of shalya treatment of basti in kaya chikitsa Being physicians it is important to know about the siras which are not to be punctured which conducting various surgical procedure to complications. So the study of Avedhya Sira is of importance .There are 700 siras.Among these  98 siras are avedhya. In sakhas  there  4 siras are avedhya 1  Jaldhara  1 urvi 2 Lohitaksha.  Urvi and lohitaksha abhyantara siras while jaladhara is a bahya sira  as the study is undertaken on upper limb the siras can be renamed as Jaldhara 1 Bahvi 1 Lohitaksha. The Classification of blood vessels are based on different criteria in Ayurveda and contemporary science so it is difficult for the exact correlation of sira for, dhamanis or other vessels with vacant space inside to any particular structure such as vein or artery .This study  a” is aimed to identify the Sirās mentioned in avedhya sira sakha of  with comparison to the blood vessels of the extremity .

Keywords: Avedhya sira ,Marma ,Rakt mokshan,Bahvi,Lohitaksha,Urvi

ABSTRACT

The present study is designed to review whether the combination therapy of Infliximab and Methotrexate is better than Methotrexate monotherapy. We have reviewed that combination therapy of TNF-  inhibitors and Methotrexate in RA. How TNF-alpha inhibitors (Infliximab) and Methotrexate performed in randomized controlled trials when compared to Methotrexate in Methotrexate naive Rheumatoid Arthritis patients.

Keywords: Cytokines and inflammatory mediators, Immunology, Rheumatic diseases, Rheumatoid Arthritis (RA), Tissues.

ABSTRACT

The growing interest in development of newer technologies to improve human health has lead to emergence of a new field called Nanorobotics. Nanorobotics is a technique in which robots of nanometer scale are created. The term nanorobot is a combination of two terms robot and nanometer. The size of nanorobots ranges from 0.5 to 3 microns in diameter. Synonyms of nanorobots are nanobots, nanoids, nanites, nanomachines and nanomites. The main element used in manufacturing of nanorobots will be carbon in the form of diamond/fullerene nanocomposite because of their strength and chemical inertness. Nanorobots may consist of molecular sorting rotors, propellers, sensors and fins. As nanorobots are of nanometer size, they work simillarly to viruses, bacteria, tumor cells and can be used to fight these threats to human body in coming future. The main feature of nanorobots will be its wide applicability in various fields. They can be used in early diagnosis and treatment of cancer and diabetes. In the field of Dentistry nanorobots can be used for oral analgesia, tooth repair, tooth alignment and diagnosis of oral cancer. Better targeted drug delivery can also be achieved in comparison of conventional devices. Other biomedical applications of nanorobots include breakdown of blood clots and kidney stones, in arteriosclerosis, nerve regeneration, parasite removal, as artificial oxygen carrier etc. The review article aims to provide an early glimpse on the structure, design, types, current scenario and future applications of nanorobots in various fields.

Keywords: Nanorobotics, Nanorobot, Nanotechnology

ABSTRACT

Cordia dichotoma Forst. (Family Boraginaceae) is a tree of tropical and sub-tropical regions, grows in the sub-Himalayan tract and outer ranges, ascending upto about 1500 m elevation. It found in a variety of places like, the dry deciduous forests of Rajasthan and moist deciduous forest of western Ghat and tidal forests in Myanmar. The common name of the plant is Lasura, Borla, Bhokar etc. Phytochemically it consists of carbohydrates, alkaloids, glycosides, flavonoids, tannins and saponins. Chemical screening of both fruit and leaves shows the presence of pyrrolizidine alkaloids, coumarines, flavonoids, saponins, terpenes and sterol. Pharmacologically proved activities are anti-ulcer, wound healing, anti-inflammatory, antioxidant, anti-diabetic and hepatoprotective activity.

Keywords: Cordia dichotoma, Hepatoprotective activity

ABSTRACT

Cancer drug development is leading the way in exploiting molecular biological and genetic information to develop ’personalized’ medicine. The therapies such as immunotherapy, gene targeted nucleic acid therapy, targeting angiogensis for treatment, chemotherapy are introduced for the treatment of cancer. In chemotherapy the drug new drug are introduced nivolumab, bevacizumab, belinostat, bilinatumomab.

Keywords:  cancer treatment, immunotherapy, chemotherapy, targeting angiogensis, nucleic acid therapy.

ABSTRACT

Transdermal delivery holds a promising carrier in the transport of drugs to get direct access across the skin deep into the systemic circulation. It has attracted many researchers due to various biomedical advantages. The barrier nature of stratum corneum poses a threat to the drug delivery. Recently, the use of microneedles in increasing skin permeability has been proposed and shown to dramatically increase transdermal delivery, especially for macromolecules. In the microelectronics industry, microneedles have been fabricated with a range of sizes, shapes and materials. Most drug delivery studies have emphasized solid microneedles, which have been shown to increase skin permeability to a broad range of molecules and nanoparticles in vitro Microneedles can be used to enhance transdermal drug delivery. In this review different types of microneedles are described and their methods of fabrication highlighted. There are also hydrogel-forming microneedles. These are innovative microneedles which do not contain drugs but imbibe interstitial fluid to form continuous conduits between dermal microcirculation and an attached patch-type reservoir. Several microneedles approved by regulatory authorities for clinical use are also examined. It also focuses on the delivery of various therapeutic agents effectively different carriers emphasizing mainly on the potential role of microneedles as transdermal system.

Keywords: Transdermal drug delivery, Injection, Needles, Permeation, Skin, Systemic circulation

ABSTRACT

Anti-fungal agents like flucanazole, itraconazole, ketoconazole, clotrimazole etc. are used to treat various superficial and systemic fungal infections. Oral and parenteral administration of the antifungal drugs are associated with various side effects including headache, nausea, vomiting, abdominal pain, gastric ulceration and bleeding. Hepatic and renal toxicity was also observed in patients on high and prolonged use of drugs. Film forming hydrogels are the dosage form for the topical delivery of drugs and it can bypass the side effects related to the conventional dosage forms and can provide effective topical release of the drugs. These film forming gels are novel approach for providing sustained release with increased residence time, therapeutic effect and patient comfort.

Keywords:  Antifungal agents, film forming hydrogel, topical drug delivery.

ABSTRACT

A new selective, sensitive and Rapid Reverse phase-UPLC method was developed and validated to determine the known potential impurities present in Telmisartan (TL) and Hydrochlorothiazide (HC) in fixed dose combination drug product. The quantification was carried out by using Acquity UPLC, HSS T3 (100 × 2.1) mm, 1.8m column, with a flow rate of  0.5mL/min at 225 nm .The mobile phase consists of 0.1% ortho phosphoric acid pH adjusted to 2.6 with diluted sodium hydroxide as Mobile phase A and acetonitrile as Mobile phase B. Separation of the impurities was achieved within 10.0 minutes of run time. Typical retention times of TL and HC were found to be about 5.4 and 2.0 minutes respectively. The product was subjected to various degradation conditions and validated in terms of linearity, precision, accuracy, LOD, LOQ and robustness in accordance with ICH guidelines. The known impurities quantified in this study were HC imp-1 to 4 for Hydrochlorothiazide and TL imp-1 to 6 for Telmisartan. Recovery was established for all the impurities with respective to LOQ to 150%. The data supports that the newly developed method is capable to determine all the potential impurities of TL and HC.

Keywords: Telmisartan, Hydrochlorothiazide, Forced Degradation, RP-UPLC and Stability Indicating

ABSTRACT

A simple, specific, quick, isocratic Reversed Phase High Performance Liquid Chromatographic method was developed and validated for the analysis of Noscapine. RP-HPLC method was developed on a Symmetry C-8 (4.6 × 150 mm), 3.5 µm particle, reversed-phase column. The mobile phase was 0.1% octane sulphonic acid (pH- 3): acetonitrile, 40:60 (v/v) at a flow rate of 0.8 ml/min. and the eluate was monitored at 260 nm. The retention time of the drug was found to be 2.314 min. The method was linear over the range of 4-8 μg/ml with a regression coefficient of 0.999 and validated with respect to accuracy, precision, linearity, and specificity, limit of detection and limit of quantization as per the guidelines of International Conference for Harmonization (ICH). This method can be used in the industries for determination of Noscapine to analyze the quality of formulation without interference of the excipients.

Keywords: Noscapine, RP-HPLC, validation, ICH.

ABSTRACT

9,10-Bicyclo-3-substituted-pyrazine-2-(1H)-one was prepared by mixing substituted  aromatic diamine and 2-oxo-2-substituteted acetic  acid in aq. HCl and then stirred at 40⁰Cfor 4 hrs. Progress of the reaction by the formation of thick solid & it was monitored  by TLC ( ethyl acetate /Hexane ,1:1) After the completion of the reaction, the solid product was filtered, washed with the water and dried .The crude product was purified by dissolving in hot aqueous NaOH followed by neutralization with acetic acid. The isolated product was recrystalised from  methyl isobutyl ketone. The compounds thus synthesized have been characterized by physical and spectral data. All of these titled synthesized compounds have been screened for antimicrobial study and  are found to possesses excellent antimicrobial activities.

Keywords : Synthesis, Characterization, biological evaluation, pyrazine

ABSTRACT

To investigate the phytoconstituents of ethanolic extract of Grewia flavescens juss whole plant using GC-MS. GC-MS analysis of Grewia flavescens juss whole plant was performed by using Agilent 6890 GC with 59739N MSD and GC -MS equipped with Elite–I fused with silica capillary column (Cpsil 8cb:30mm×25mm×0.25mm).The result of GC-MS analysis confirmed the presence of 12 compounds. The most prevailing compounds are Ethanamine, N,N-dimethyl, Acetic acid, Ethane,1,1-diethoxy-, Pyridine, Diethyl phthalate, Ethyl. alpha-d-glucopyranoside, 4-((1e)-3-hydroxy-1-propenyl)-2-methoxyphenol, n-hexadecanoic acid, hexadecanoic acid ethyl ester, Desaspidinol, Phytol, and Octadecanoic acid. The presence of phytoconstitutents reveals the presence of medicinal value.

Keywords: Grewia flavescens juss whole plant, Ethanolic Extract, GC-MS analysis.

ABSTRACT

A tattoo is a form of body modification by inserting indelible ink into the dermis of the skin to change the pigment. Permanent makeup is a cosmetic technique which employs tattoos as a means of producing designs that resemble makeup. In the United States, the percentage of adults with minimum one tattoo has increased from 21% in 2012 to around 38% in 2016. The process of tattooing exposes the recipient to risks of infections with various pathogens, which are serious and difficult to treat. Other risks include allergic reactions, swelling and burning, granulomas, keloid formation and complications with MRI. Removal of tattoo is cumbersome. The pigments used in the inks are color additives, which are subject to premarket approval under the Federal Food, Drug, and Cosmetic Act. However, because of other competing public health priorities and a previous lack of evidence of safety problems specifically associated with these pigments, FDA traditionally has not exercised regulatory authority for color additives on the pigments used in tattoo inks. FDA only monitors problems from tattoos and permanent make-up and alerts the public when they become aware of a problem. Consumers should be aware of the risks involved in order to make an informed decision. FDA urges consumers and healthcare providers to report adverse reactions from tattoos, permanent makeup, and temporary tattoos, as well as problems with tattoo removal. But it’s high time that FDA takes a strong call on this matter and strictly regulates these practices to prevent further harm to public.

Keywords: Tattoo, US-FDA, Permanent Makeup, Regulations

ABSTRACT

Isoamyl-2-cyanoacrylate is a non-toxic, bio-compatible, haemostatic and bacteria static monomeric component in nature. But in presence of moisture it gets converted into polymer. It is used as tissue Bio-adhesive; it is an alternative to suturing in medical and cosmetic surgeries. It is an inert material solidifies rapidly in alkaline media and slowly solidifies in acidic media within 5-10 seconds. It has a tendency of rapid wound closure with minimal scarring and reduces the subsequent infection. It is less traumatic and more efficient, precise and safe. It effectively replaces the conventional wound closure procedures. It is an active component in brand name “Amcrylate” is manufactured and promoted by” Concord drugs Limited” Hyderabad. The analytical gas chromatographic method is developed for the estimation of purity of isoamyl-2-cyanoacrylate, procedure as follows.

Keywords: Iso Amyl 2-CyanoAcrylate, Bio-Adhesive, Suture less Skin closure in Pediatric day-care surgery, Amcrylate Purity Analysis by Gas-Chromatography.

ABSTRACT

The main focus of the present study was to explore co-crystallization technique to engineer pharmaceutical co-crystals of poorly aqueous soluble drug- Gliclazide (GLZ) using different GRAS listed coformers; benzoic acid (BA) and itaconic acid (IA). The complexation energy of GLZ and coformers were predicted by Quantum Mechanics method. Co-crystals in 1:2 molar ratios were formulated using solvent evaporation technique using acetone, a class III solvent as a medium for drug and coformer interaction at molecular level. The characteristics of GLZ and resultant co-crystals were evaluated in terms of flowability, drug content uniformity, saturation solubility and in-vitro dissolution studies. Further Fourier transformation infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscopy (SEM) were used to identify hydrogen bonding interaction, melting point, crystallinity and surface morphological characteristics of prepared co-crystals respectively. The obtained GLZ co-crystals indicated presence of additional peaks as well as band shifts in the infrared spectrum. Additionally DSC thermograph and XRD confirmed change in crystal lattice. The results of in-vitro dissolution indicated a significant enhancement in the dissolution profiles of both the co-crystals as compared to GLZ. Thus it could be concluded that the co-crystallization technique could be successfully exploited to develop new formulation of GLZ.

Keywords: Gliclazide, Coformers, Co-crystals, Complexation energy, Quantum mechanics, Solvent evaporation.

ABSTRACT

The objectives of this study was to examine the antioxidant activities of aqueous extracts of bark of Psidium guajava bellowing to family Myrtaceae, which is originated in Mexico and extends all over the South America, Europe, Africa and Asia. The Psidium guajava is used traditionally  for the treatment of various ailments like  antioxidant, hepatoprotective, anti-allergy, antimicrobial, antigenotoxic, antiplasmodial, cytotoxic, antispasmodic, cardioactive, anticough, antidiabetic, anti-inflammatory and antinociceptive activities. For the antioxidant activity of aqueous extract of bark of Psidium guajava Linn, In-vitro and In-vivo methods are used. In-vitro assessment of the ability of the extract to scavenge the Hydrogen peroxide (H₂O₂) was determined with reference to the synthetic antioxidant vitamin C and ascorbic acid was used as standard antioxidants. The scavenging activity of plant extract on hydrogen peroxide was found similar as scavenging activity of vitamin C. The Psidium guajava showed the strong In-vitro antioxidant activity and exhibited over 86.01% inhibition at 12 µg/ml concentration. For In-vivo antioxidant activity catalase (CAT) enzyme level was used. CAT levels were measured in fresh liver tissue using ELISA. CAT in hepatic tissue compared to control group. CAT enzymes were significantly increased when treated with aqueous extract of bark of Psidium guajava. In human beings, the highest levels of CAT are found in the liver, kidney and erythrocytes, where it is believed to account for the majority of H₂O₂ decomposition. These results show that the Psidium guajava could be considered as a natural antioxidant source.

Keywords: Antioxidant activity, Psidium guajava Linn, catalase activity, Hydrogen peroxide, aqueous extract.

ABSTRACT

Imidazo [1, 2-a] pyridine based Schiff bases have been synthesized by condensing different 3-aryl-5-methyl isoxazole hydrazides with 2-aryl imidazo [1, 2-a] pyridine carbaldehydes by following hybridization approach. The structures of newly synthesized Schiff bases have been characterized by spectral data and elemental analysis. In In vivo anti-inflammatory screening, compounds 4b & 4f showed significant activity and the results are comparable with the standard drug, diclofenac. None of the compounds exhibited significant activity in anti-bacterial study. The work might result in the emergence of new series of compounds with potent anti-inflammatory activity.

Keywords: Imidazo [1, 2-a] pyridines, isoxazole hydrazides, Schiff bases, anti-bacterial activity, anti-inflammatory activity

ABSTRACT

Cancer is deliberate to be caused by the interaction between genetic susceptibility and environmental toxins. Based on the DNA changes in cells, proliferating cycle of tumor cells can be divided into 4 phase’s Pre-synthetic phase (Gap 1 phase or G1 phase). The antiproliferative activities of these compounds were evaluated against a Cytotoxicity analysis of compounds against leukemia cell line -K562 organism homo sapiens (human) organ bone - marrow.Tissue - lymphoblast, disease - chronic myelogenous leukemia (CML) one human tumor cell lines (K562) by applying the MTT colorimetric assay. The 1, 3-disubstituted urea derivatives show good antiproliferative activity against human cancer cell lines (K562). Generally, an aromatic ring on N-3 seems to be in favor of enhancing the inhibitory activity, compounds introduced a Nitro group substituted at C-3 position on the aromatic ring approved to generally decrease    activity. Cells were incubated with different concentrations of the extract for 5 days in a 96 well plate, after which the liver cells which did not take in stain and dead cells which took in stain were counted. For counting the cell suspension was mixed with an equal volume of trypan blue and was counted. A concentration that inhibited the growth of cells at 50% (IC50) was computed. Substances with low IC50 indicate potential for cytotoxicity. (A) 1, 1-dimethyl-3-phenyl-3-(5-phenyl-1, 3, 4-thiadiazol-2-yl) urea was found higher activity

Keywords: Cancer, urea derivative, antiproliferative activities, malignant behavior.

ABSTRACT

A new simple, accurate, rapid and precise isocratic RP-HPLC was developed and validated for the determination of Rosuvastatin and Ezetimibe in Pharmaceutical tablet dosage form by droping method. The Method employs Shimadzu LC system on Hypersil ODS column (4.6 x 250 mm, 5 µm) and flow rate of 1.5ml/min with an injection volume 20µl.  Buffer, Acetonitrile and Methanol was used as mobile phase in the composition of 40:30:30v/v. The Detection was carried out at 230nm. Linearity ranges for Rosuvastatin and Ezetimibe were 11-33µg/ml, 10-30µg/ml respectively for HPLC. Retention Time of Rosuvastatin and Ezetimibe were found to be 3.7 and 5.7 min respectively. Percent Recovery study values of Rosuvastatin and Ezetimibe were found 99.6-101.1% and 99.9-100.7% respectively. This newly developed method i.e. droping method was successfully utilized for the Quantitative estimation of Rosuvastatin and Ezetimibe in tablet dosage form. This method was validated for selectivity, accuracy, precision, and linearity, Ruggedness, Robustness and Stability Studies as per ICH guidelines.

Keywords: Liquid Chromatography; Rosuvastatin, Ezetimibe, Simultaneous estimation, Validation.

ABSTRACT

The major objective of any dosage form development is to ensure the delivery of specific and reproducible amounts of pharmacologically active compounds to the body in the maximum amount possible. Today's most frequently used dosage forms are orally administered solids formulated such as tablets, capsules or powders. Timed-release products intend to improve delivery efficacy and/or effectiveness; for instance, the frequency of dosing can be reduced and, in certain cases, the actual daily dose can be reduced, offering the manufacturer a financial benefit. There have been many techniques developed for producing the variety of timed-release products. Ginger is a natural drug, which is used for nausea and vomiting, to treat bleeding disorders and rheumatism. In conventional dose is thrice a day, 8-10 gm which is not at all convenient for the patient. Increase the patient compliance is also a great challenge which is continuously improving by the novel drug delivery system. The main objective of the present work is to design Ginger root extract powder (5%w/w of 6-gingerol) timed release dosage form of the drug with the help of a novel clear transparent veggie capsule shell of ‘0’ size made up of cellulose and natural substance. The objective in formulating a sustained release dosage form is to be able to provide a similar blood plasma level pattern for up to desired hrs (12hrs) after oral administration of the drug. The formulation, optimization, destructive quantification parameters and in-vitro studies of the drug have focused in this research article. The presented work sought a futuristic research for the benefit of the patients.

Keywords: Sustained Release, Timed drug delivery, Novel drug delivery, Veggie Capsules

ABSTRACT

Synthesis of certain new fused 1,4-diazepine derivatives, namely, cyclopentathienodiazepinones and their benzothieno analogues IV to produce new compounds of possible CNS depressant activity. Eleven compounds IV 1, 5, 6, 7, 12, 13, 15, 19, 20, 21 & 26 were selected and submitted to pharmacological evaluation for anxiolytic and tranquilizing activity in the open field test.

Keywords: 1,4-Diazepine derivatives, Open-Field test, Anxiolytic and Tranquilizing Activity

ABSTRACT

The present study was undertaken to identify the active principles in leaf, Stem and Root extracts of Ruta graveolens L. using gas chromatography-mass spectrometry (GC-MS). The plant material was extracted in methanol by using Soxhlet apparatus for 24 hours and the extracts were analyzed using GC-MS. The mass spectra of the compounds observed were matched with the National Institute of Standards and Technology (NIST) library. The results revealed the presence of 17, 12 and 6 chemical compounds in leaf, stem and root extracts respectively. The major chemical constituents were kokusaginine (39.9%), Bergaptene (25%),2-Undecanone (14.97%),1-(1,3-Benzodioxol-5-ylmethyl)-3-Nitro-1(12.69%),Pyrrole-3-carboxaldehyde,1-(4- methoxyph(9.36%).Some of these compounds have been reported to possess various bioactivities such as anti-microbial, anti-viral, anti-oxidative, anti-proliferative, anti-inflammatory, anti-tumour,etc. The study is a base to understand the richness of bioactive components in methanolic extracts from different parts of Ruta graveolens L. Their isolation would have potential applications in drug designing as well as in the medicine and healthcare industries.

Keywords: Ruta graveolens, active principles, Gas Chromatography-mass spectrometry (GC-MS).

ABSTRACT

Nutrition has been clearly identified as a key factor in Human development, not only as a conditioning factor for health but also as a determinant of quality of throughout the life cycle, malnutrition affect not only mortality and morbidity figures, but also growth protein deficiency also affect growth and wellbeing of human Present study taken for treatment of protein deficiencies by isolating proteins from soya beans and formulate them in suitable dosage form.

Keywords: Soya beans, Soy protein isolation.

ABSTRACT

The present study includes the Formulation and Evaluation of Mucoadhesive Buccal Patch of Timolol Maleate for this study work timolol maleate selected as model drug and using either ionic polymers (SCMC) or non-ionic polymers (carbopol, HPMC).The fabricated patches were prepared by solvent casting method.  The mean thicknesses of the buccal patch formulations were 0.34 – 0.43 mm. Moisture uptake of transdermal patches were found to be 2.94-4.13.which prevents the patches from microbial growth and bulkiness. As amount of PVP increased in every polymer blend, tensile strength and elongation at break were increased. Addition of PVP predominantly decreased the swelling characteristics of the buccal patches, except for SCMC. The drug content of the prepared bioadhesive buccal patches were found in the range of 91.4 - 98.54 %.Bioadhesive strength of buccal patches in following order SCMC >Carbopol>HPMC. The release of Timolol maleate from HPMC patches was slower than SCMC and CP 934.As PVP concentration increased, dissolution rate increases among all polymers. For determination of λmax the solution of the timolol maleate was subjected to ultraviolet scanning in the rage 200 to 400 nm. The λmax was found to be at 294 nm .The pH of formulations was found to be 6.8 - 7.5 which is within the limit of semisolid specifications. The folding endurance of BP formulations was found to be 296 – 325.The results indicated that all formulations were flexible and soft. Bioadhesive buccal patches containing SCMC, HPMC and Carbopol showed a zero order drug release.

Keywords: Timolol Maleate, Mucoadhesion, Buccal Patch, PVP, HPMC.

ABSTRACT

Pharmaceutical R&D is failing with an era of triple obstacles – increased timelines for approval, high cost and even higher failure rates. The world around us is constantly putting pressure on creating completely new solutions for about 4000 diseases with known molecular basics and many other diseases without basic intellect. There comes a need to remove the wide gap in innovation showcasing a challenge for drug discovery. The shockingly tedious drug development process is forcing us to find more effective solutions and drug repurposing can be a starting point where the clear understanding of the de novo pathway for an existing drug essentially unlocks the full potential for repurposing a drug for other diseases. Drug repositioning (also known as drug repurposing, re-profiling, re-tasking or therapeutic switching) is the application of known  drugs and compounds to new indications (i.e., new diseases). This idea dates back with cases like Viagra, Thalidomide, and Aspirin etc. There are a number of approaches to drug repurposing, but these are ultimately an expedition into new area. Scientists have to justify examining a compound in a different disease state, so they often make a hypothesis based on possible associations between mechanisms. A significant advantage of drug repositioning over traditional drug development is that since the repositioned drug has already passed a significant number of toxicity and other tests, its safety is known and the risk of failure for reasons of adverse toxicology are reduced. The possibilities are endless, and animal models are elevating drug repurposing's potential.

Keywords: Drug Repurposing, New indications, de-novo pathway.

ABSTRACT

The present study investigates the chemical composition of essential oil of leaves of Tridax procumbens (L.) and its invitro anticancer activity.  Traditionally, the plant is used for malaria, stomachache, high blood pressure, hemorrhage and to prevent hair fall as well. It possesses antifungal, antibacterial, antiseptic, insecticidal, parasiticidal and hepatoprotective properties. The hydrodistilled essential oil of T.procumbens contains total of 18 components by GC-MS analysis. Dibutyl phthalate (19.29%), Trans-(α)-caryophyllene (9.55%), Biformeme (3.95%), p-cymen-7-ol (2.52%), 1,8-cineole (2.44%). And the minor compounds are trans-α- Bergamotol (1.78%), 2-α-pinene (1.62%), α-Selinine (1.49%), Caryophyllene oxide (1.39%), α-humulene (0.95%),  The obtained essential oil was tested against Human breast cancer cell line (MCF-7) for its anticancer activity by MTT assay with different concentrations of essential oil (18.5-300 µg/ml). The result revealed that the essential oil showed concentration dependent activity against cell line. The IC₅₀ value of MCF-7cell line was 96.6 µg/ml. This may be due to the presence of important terpenes present in the oil. There are only few reports are available for anticancer activity efficacy of this plant. Our findings confirm the anticancer potential of the T.procumbens.

Keywords: T. procumbens, Dibutyl phthalate, Trans-(α)-caryophyllene, Biformeme and MCF-7

ABSTRACT

An 18 years old male patient with history of RVD (+ve) on ART reported generalized weakness, body pains, head ache, and loose motions 3 episodes since one week. Acute pancreatitis due to anti-retro viral therapy was diagnosed. Lamivudine was most probable causal agent. Pancreatitis was confirmed by ultra sound scan of abdomen.

Keywords:  Lamivudine, Pancreatitis, Anti-retro viral therapy, Patient care.

ABSTRACT

Bivalve shells are covered with a hard part which is made up of calcium carbonate (CaCO₃). The bivalve shells  have wide applications among one is a partial replacement of mortar. In this study, Yadayanthittu estuarian Meretix casta shells have experimented for partial replacement in the mortar. A variety of experiments were conducted and the results are discussed in details. The estuarian M.casta (bivalve) shells chemical constituents were measured by XRF instrument. The analytical results demonstrate that the Meretrix casta shells having a loss on ignition (LOI) about 44.00%; the calcium oxide (CaO) occupy 54.47%, and the other reported oxides accumulated to 1.5287 %. For mortar replacement study,  a total of seven experiments (E1-E7) was performed with different combinations. The first combination (E1) without any replacement in mortar and the second (E2) with 12.5% of fly ash replacement and the remaining experiments (E3-E7) consist of  Meretrix casta shell powder (MCSP) with various proportions of 12.5%, 8.75%, 8.33%, along with fine aggregates. Each combination was mixed with water and casted separately. After 07 and 28 days of curing, they cubes were removed, dried and measured the compressive strength. The compressive strength results indicate that the E7 combination exhibits higher strength by 41.80 and 56.8 Pa respectively. This could be due to the C-S-H gel formation in the mortar. The lowest results are observed in E4 combination, with the compressive strength of 32.42 and 47.42 at the age 07 and 28 days. These experiments show not enough binding capacity may be due to inadequate C-S-H gel formation. 

Keywords:  Yadayanthittu estuary, Meretrix casta shells, chemistry, mortar, compressive strength.

ABSTRACT

Diabetes Mellitus is a metabolic disorder characterized by high blood glucose level caused by deficiency of insulin secretion or insulin action. Postprandial blood glucose level in patients with type II diabetes may be controlled by inhibition of alpha amylase, which is one of the carbohydrate hydrolysing enzymes. Alpha amylase is an enzyme which breaks down starch to maltose by hydrolysing alpha bonds of large, alpha-linked polysaccharides, such as starch and glycogen. Alpha amylase inhibitors may be useful as adjuvant drugs in type II diabetes. The objective of this review is to gather information regarding the identification and evaluation of alpha amylase inhibitors from natural and synthetic sources.

Keywords: Alpha amylase, antidiabetic.

ABSTRACT

In this current research work the nanoparticles containing Cyclophosphamide using natural Gumghatti as a polymer has been formulated for the enhanced anticancer activity. The nanoprecipitation method has been utilized for the preparation of Cyclophosphamide comprising natural Gumghatti as polymer. The prepared nanoparticles have shown the average particle size, polydispersity index and zeta potential of 143.4 nm, 0.16 and 28.5 mV respectively. Further the encapsulation efficiency, percentage drug loading and percentage yield for all the formulations were substantial, especially for the trial 6 the values observed were 93.56, 83.55 and 76.54 respectively. The invitro release of Cyclophosphamide Gumghatti nanoformulations and were determined by dissolution tester by USP apparatus II in 900ml phosphate buffer pH 6.8. The dissolution media were maintained at 37±0.5°C with a paddle rotation speed at 50 rpm. The amount of drug used was equivalent to 15 mg at specified time intervals (5, 10 15, 20, 25 30 60, 90 and 120 minutes.) The results shows that prepared nanoparticles having 98.53 % of drug release in 120 minutes, further it indicates more than 95 % of drug release in 2 hours. Invivo anticancer activity has been performed using Swiss albino mice, the results indicated that the enhanced anticancer activity of the prepared nanoformulations.

Keywords: Cyclophosphamide, Gumghatti, Nanoprecipitation, invitro drug release, anticancer activity.

ABSTRACT

Right Ventricular Infarction was first recognized in a subgroup of patients with inferior wall myocardial infarctions who demonstrated right ventricular failure and elevated right ventricular filling pressures despite relatively normal left ventricular filling pressures. The classical triad of right ventricular infarction includes distended neck veins, clear lung fields, and hypotension. We present a case report of a 48 years old male patient, a known hypertensive for 9 years, a heavy smoker for more than 10 years, also a known Gout patient, who was admitted at Wuhan union hospital department of cardiology, who presented with the chief complain of severe left sided chest pain interfering with his daily activities, which was associated with dizziness and diaphoresis, Blood pressure on admission was 80/50mmHg(hypotension) his heart rate was 99b/min, and clear lung fields on auscultation, clinical and imaging findings suggestive of Right ventricular infarction. Increasing recognition of Right ventricular infarction either in association with left ventricular infarction or as an isolated event, emphasizes the clinical significance of the right ventricle to total cardiac function, thus it is really important to have knowledge on how to diagnose RV infarction and reminding ourselves particularly through case reports because of the therapeutic implications of distinguishing patients with right ventricular dysfunction from those with the more usual clinical presentation of left ventricular dysfunction.

Keywords: RV infarction, hypotension, distended neck veins, clear lung fields, RVMI-Right ventricular myocardial infarction

ABSTRACT

A burn is a wound in which there is coagulative necrosis of the tissue, majority of which are caused by heat. Burn injury is a major public health problem in many areas of the world. Infection in burn wounds is the second most common cause of mortality in burn cases after pneumonia. Burns predispose to infection by damaging the protective barrier function of the skin, thus facilitating the entry of pathogenic microorganisms. Burn itself is an immunocompromised condition. The present study was therefore undertaken to isolate and identify the aerobic bacterial flora in burn patients and its antibiotic susceptibility pattern. A total of 100 patients admitted with different degree of burns were studied. Wound swabs were taken with aseptic precautions by dry sterile cotton swab sticks. These swabs were transported to the microbiology laboratory and isolates were identified by standard microbiological methods. Antibiotic susceptibility was done by Kirby Bauer’s Disk Diffusion method as per CLSI (Clinical and Laboratory Standards Institute ) guidelines. A total of 120 bacterial pathogens were isolates from 100 patients. Out of them 70  are monomicrobial in and 20 are polymicrobial in nature. The most frequent cause of infection was found to be Staphylococcus aureus (33.33%), followed by Pseudomonas aeruginosa (29.67%), Klebsiella pneumoniae (17.5%), E.coli (13.33%)  Citrobacter spp (4.1%) and Proteus spp. (2.94%). Out of the total Staphylococcus aureus isolates, 55% were Methicillin sensitive and 45% were Methicillin resistant (MRSA). All the MRSA strains were 100% sensitive to Vancomycin and Linezolid. The Pseudomonas aeruginosa isolates were most sensitive to Imipenem (97%), Amikacin (57%), Pipercillin (57%) , Ciprofloxacin (54%) and Ceftazidime (34% ) Staphylococcus aureus and Pseudomonas aeruginosa were major causes of infection in burn wounds. Therefore it is necessary to implement urgent measures for restriction of nosocomial infections, sensible limitation on the use of antimicrobial agents, strict disinfection and hygiene.

Keywords: Burn wound infection, Antibiotic susceptibility testing, MRSA

ABSTRACT

Sensitive spectrophotometric method is described for the determination of tetracycline HCl in bulk and in pharmaceutical formulations. The method is based on the coupling of tetracycline HCl with diazotized 8-hydroxy quinoline reagent in basic medium at room temperature to form a reddish to brown mono azo dye soluble in water with maximum absorption at 395 nm. The reaction was followed up spectrophotometrically by measuring the increase in absorbance at 395 nm. The analytical performance of the method, in terms of accuracy and precision, was statistically validated; the results were satisfactory. The calibration graph is linear in the concentration range 1-20 μg ml^-1 ,with 0.005 μg ml^-1 detection limit and 0.324 μg ml^-1 , 0.980 μg ml^-1  Limit of detection(LOD) and Limit of quantification(LOQ) respectively. The method has been successfully applied to the determination of the studied drugs in commercial pharmaceutical formulations.

Keywords: Spectrophotometric method, Validation ,Tetracycline HCl, Coupling reaction.

ABSTRACT

Aldose reductase (ALR2; AR; EC 1.1.1.21) is the first enzyme of the polyol pathway, which reduces glucose to sorbitol, in the presence of NADPH. The pathway is completed by sorbitol dehydrogenase, which catalyzes the NAD-linked oxidation of sorbitol to fructose. Synthesis and accumulation of sorbitol in cells due to increased aldose reductase activity is one of the main causes of diabetic complications. The aim of our study is to determine the potential inhibitory effect of some 2, 4-TZD derivatives on aldose reductase enzyme activity. Aldose reductase enzyme is isolated from bovine lenses and the activity of the enzyme is determined by spectrophotometric method. In our study 13 thiazolidinedione (TZD) derivatives which are containing benzyl and phenacyl groups were studied. Maximum inhibitory activity was found with 2,4- TZD-N-unsubstituted compound (86 %).  Compound 13, unsubstituted compound which was showed the maximum inhibitory activity, will be the key formula of our future studies.

Keywords: Aldose reductase, polyol pathway, 2,4- thiazolidinedione derivatives

ABSTRACT

Neurodegenerative disorders are conditions in which cells of the brain and/or spinal cord degenerate.  The brain and spinal cord are composed of neurons with different functions such as controlling skilled movements, processing sensory information, storage of information and making decisions. Cells of the brain and spinal cord do not usually regenerate, so damage to the nervous system can be devastating. Normally, the neurodegenerative process begins long before any symptoms appear. Neurodegenerative diseases result from deterioration of neurons or their myelin sheaths which over time will lead to dysfunction and disabilities. Neuro-degenerative diseases markedly affect the lives of millions and lead to a growing public health challenge with increased costs for individuals and society. The prevention and treatment of these neurodegenerative disorders represent a critical goal of medical research today. Most of these disorders increase with age. Today, there are 25 million suffering from dementia and it is generally believed that the prevalence will be 130 million demented persons by 2050. As the human outer skin proved it to be the largest organ of sense of body, that can be potentially used for the delivery of multiple therapy for the successful management of neurobehavioral disorders. Various novel approaches can be introduced for which further study is essential .The focus on this route has not been in limelight till yet. Transdermal drug delivery is helpful for topical and local action of the drug. . For the patients who have difficulties swallowing solids or liquids, a transdermal drug delivery may offer great advantages over conventional delivery methods. Drug delivery directly to the brain interstitium has recently been markedly enhanced through the rational design of polymer-based drug delivery system. After the oral administration of drugs, the huge variations were associated in plasma levels with regular gastintestinal symptoms including nausea, vomiting, diarrhea, constipation, anorexia, abdominal pain and abdominal distention. This drug administration route could therefore allow optimal therapeutic dose, potentially further improving the effectiveness of treatment. The transdermal delivery bypasses the first past metabolism and lesser side effects. This route may be explored for the delivery of nano-sized pharmaceuticals to the CNS as an alternate route.

Keywords: Parkinson’s disease, Neurological behaviors, BBB, Nanotechnology, Skin.

ABSTRACT

A modest, fast, precise, and accurate, stability-indicating reversed phase high performance liquid chromatographic method was developed and validated for vierodt’s method of analysis  of rosuvastatin calcium(RSTC) and fenofibrate (FBT). The  volume of injection sample was 20 μl and the quantification was obtained by UV-VISIBLE detector at 240nm.The chromatographic separation was achieved on X bridge C₁₈, 250 x 4.6 mm, 5 µm particle column, by an gradient mobile phase comprising of acetonitrile: 10 mM potassium dihydrogen phosphate buffer solutions of pH 5.5 in the ratio of 90:10 v/v at a flow rate of 1.5 ml/ min. The retention times for RSTC and FBT were found to be 4.35min and 7.75 min, respectively. The drugs were shown to thermal, photolytic, hydrolytic, and oxidative stress conditions and the stressed samples were evaluated by the suggested method. Validation of the method was approved as per International Conference on Harmonization (ICH) guidelines. Linearity was accepted for RSTC and FBT in the range of 0.040-0.120 mg/ ml and 0.016-0.048 mg/ ml, respectively. The limits of detection were 0.02 μg/ ml and 0.05 μg/ ml, respectively and the LOQ value 0.1 μg/ ml and 0.09 μg/ ml, for RSTC and FBT, respectively. The developed method was profound to be accurate, precise and stability-indicating as no interfering peaks of degradants and excipients were identified. The suggested method is hence appropriate for application in quality-control laboratories for quantitative determination of both the drugs individually and in combination, since it is simple and rapid with good accuracy and precision.

Keywords: Rosuvastatin calcium (RSTC), Fenofibrate (FBT), reversed-phase HPLC, stability-indicating assay, forced degradation studies, method validation

ABSTRACT

Liposome are the concentric bilayer means core of center in which aqueous volume entirely envelope by the phospholipids bilayer used to transfer enzymes, protein and drugs to targets cancer cell or tissue. These are chemical moieties in which action towards target organ. It was first discovered by 1965 and soon was proposed drug delivery system. There are numerous application like anti fungal, anti cancer, anti inflammatory and anesthetic drugs. The magic bullet concept of Paul Ehrlich through very late, offers a logical solution to the age old problem unrelated and unwanted effect of therapeutic agent and optimizing the drug therapy in its true sense. Drugs would be targeted by virtue of groups having affinity for specific cells, tissues or organs. Liposome having also its modifications or upgraded versions likes enzymosomes, hemosomes, virosomes, and erythrosomes. Liposome has emerged as a dynamic mode for targeted drug delivery. Ligands confer specificity on a non specific reagent. Although controlled and sustained drug delivery can be considered as the magic bullet concept. We can look forward to many more clinical products in the future.

Keyword: Liposome, Magic bullet, Controlled drug delivery system, Cancer target, Bio-carrier.

ABSTRACT

Nanocochleates are unique novel drug delivery system in which, the desire drug molecule gets encapsulated into the multilayer of lipid crystal matrix. The nanocochleates structure provides protection to encochleated molecules from the degradation. It composed of negatively charged lipid generally phosphatidylserine and calcium. The nanocochleate structure has potential to carry the molecules which are hydrophobic, positively charged, negatively charged and that possess poor oral bioavailability. Nanocochleates is having more advantages than that of other dosage forms and system and hence it represents a new technology for oral and systemic delivery of drugs.

Keywords: Nanocochleates, Encochleated, Oral bioavailability, Systemic delivery.

ABSTRACT

Liposome proved themselves as a promising novel delivery vehicle of drugs to the skin, is a topic of considerable current interest. Liposomes are acceptable and superior carriers having ability to encapsulate both hydrophilic and lipophilic drugs and protect them from degradation. Liposomes are result of self-assembly of phospholipid in an aqueous media resulting in closed bilayer structures. Liposomes are one of unique drug delivery system which can be used in controlling and targeting drug delivery system. Liposomes are generally classified based upon structure, method of preparation, composition and application, conventional liposome, and specialty liposome. Different marketed formulations are available in market for liposomes. The liposomes have many applications which increase its importance over other formulations. The entrapped compound’s solubility and partitioning characteristics will determine its location in the liposomal bilayer .It also has affinity to keratin of horny layer of skin and can penetrate deeper into skin hence give better absorption. But they may also have the property into the skin, carrying actives to the target site, where these molecules will be released. Reformulation of drugs in liposomes has provided an opportunity to enhance the therapeutic indices of various agents. This review discusses the potential advantages in topical drug delivery, basic structure characteristics and mechanism of action of liposomes and evaluation parameter for liposome formulation.

Keywords: Liposome, penetration, skin, enhanced efficiency.

ABSTRACT

Lyophilization is promising approach to increase the shelf life of liposome. The major limitation in the widespread use of liposome is its instability. The aim of this study was to investigate the effect of lyophilization either in the presence or in the absence of lyoprotectant on liposome properties Lyophilization is used to ensure an increased shelf life of liposomes by preserving them in dry state more stable than the aqueous dispersion. When stored as aqueous system the encapsulated drugs are released & the liposome might aggregate or fuse. The process of lyophilization without cryoprotectant resulted in particle size increased & significant content leakage. This review work suggests that the investigation of stability of lyophilized liposomes containing PC (Phosphatidyl Choline) & cholesterol. Liposomes sphere-shaped vesicles consisting of one or more phospholipids bilayer in which both hydrophilic & hydrophobic drug entity can be incorporated. Due to their size & hydrophobic & hydrophilic character liposomes are promising for drug delivery. This structure turns liposomes into ideal drug carriers, since hydrophilic drugs tend to entrapped in the core; while hydrophobic ones will be entrapped within the lipid bilayers. Liposome is one of the most successful drug delivery system applying nanotechnology to potentiate the therapeutic efficacy & reduce toxicities of conventional medicines. The encapsulation efficiency partially depends upon the logP of drug. Lyophilization is a strategy often employed to improve liposomal formulation stability, due to reactivity being far less pronounced in the solid versus aqueous state.

Keywords: Lyophilization, liposome, cryoprotectant, stability, increased shelf life.

ABSTRACT

The purpose of writing this review article on gastro- retentive drug delivery systems (GRDDS) have been developed; the principle mechanism of floatation to achieve gastric retention. The recent developments of (FDSS) including the physiological and formulation variables affecting the gastric retention. Several techniques such as floating drug delivery system, low density systems, raft systems, mucoadhesive systems, high density systems, super- porous hydro- gels and magnetic systems, have been employed. Floating drug delivery systems have a bulk density less than gastric fluids and so, remain buoyant in the stomach for a prolonged period of time, releasing the drug slowly at the desired rate from the system. Dosage forms available as gastric floating systems include tablets, capsules, granules and microspheres.

Keywords: Floating tablet, Gastro- retentive drug delivery system, Gastric resistance time, Rosuvastatin calcium.

ABSTRACT

A new, simple, specific, accurate and precise RP-HPLC method was developed for determination of Baclofen. In the present study, stress testing of Baclofen was carried out according to ICH guidelines Q1A (R2). Baclofen was subjected to stress conditions of hydrolysis, oxidation, photolysis and neutral decomposition. Extensive degradation was found to occur in acidic, condition. Mild degradation was observed in basic and at thermal conditions. Successful separation of drug from degradation products formed under stress conditions was achieved on a Hypersil BDS C18 column (250 mm × 4.6 mm, 5.0 μ particle size) using acetonitrile: acetate buffer (pH 3.7 ± 0.05) (50:50 v/v), at a flow rate of 1.0 mL/min and column was maintained at 40˚C. Quantification and linearity was achieved at 272 nm over the concentration range of 5 - 100 μg/mL for Baclofen. The method was validated for specificity, linearity, accuracy, precision, LOD, LOQ and robustness.

Keywords: Stability-indicating, HPLC, Baclofen, Validation, Stress Testing.