ABSTRACT

Chemometrics is the use of mathematical and statistical methods to improve the understanding of chemical information and to correlate quality parameters or physical properties to analytical instrument data. It is a data-driven multidisciplinary science that allows maximum collection and extraction of useful information from the analytical data of numerous application areas such as chemistry, biochemistry, medicine ,biology and chemical engineering. This review focuses mainly on numerous chemometric models used and their relevant applications in the field of pharmaceutical sciences.

Keywords: Chemometrics, analytical data, multidisciplinary science, pharmaceutical sciences.

ABSTRACT

The main purpose of this review is to highlight the importance of colorimetric approaches to drug analysis both in dosage forms as well as biological samples. Colorimetric methods using colorimetric reagents are highly sensitive, specific and an easy way of determining various analytes in a variety of matrices within a short time. The colorimetric procedures discussed are statistically validated and reported in various quality control laboratories. Hence in the present review significance of colorimetric procedures, various reagents used along with principles and applications are mentioned.

Key words: Colorimetric approaches, sensitive, matrices, quality control, applications.

ABSTRACT

Gastro Retentive Drug Delivery System is one of the novel approach and all researchers in pharma industries are focused in the same. The main aim of writing this review on Gastro Retentive floating drug delivery systems is to assemble the recent literature with special emphasis on its principal mechanism of floatation to achieve gastric retention and its recent development. Floating systems are low density systems that has density lower than gastric fluid and floats over the gastric fluid and remains buoyant in the stomach without affecting the gastric emptying rate for a prolonged period of time. Floating dosage forms can be formulated as tablets, capsule. This review article includes detailed information about its classification, advantages and in-vitro evaluation parameters.

Keywords: Gastro Retentive, Floating dosage.

ABSTRACT

Oral Lichen Planus (OLP) is a chronic inflammatory disease that affects the mucous and cutaneous tissue inside our mouth. It is a T cell mediated autoimmune disease. The two major types of OLP are Reticular OLP and Erosive OLP. They appear as white, lacy, patches, red coloured, swollen tissues or open sores. Its cause is unknown. The oral lichen planus do not pass from one person to another. This disease may be sometimes responsible for developing mouth cancer. Proper monitoring is needed for the patients who are having oral lichen planus. Personal oral hygiene is believed to reduce the symptoms of OLP. The topical or systemic corticosteroids modulate the patient’s immune response. The natural treatments by using aloe vera, yogurt, turmeric, almonds, baking soda and lemon are very much effective in treating OLP. The commonly used homeopathic medicines used for the treatment of OLP are plantaga, mercsol and borax. The non pharmacological approaches used for treating OLP include PUVA therapy, laser therapy, cryotherapy and CO2 laser. Nowadays modalities like retinoids, dapsone, hydroxychloroquine, calcineurin inhibitors and mycophenolatemofetil are used for treatment.

Keywords: oral lichen planus, corticosteroids, basal keratinocytes, immunosuppressant.

ABSTRACT

Hydrogels are three-dimensional, hydrophilic & polymeric networks capable of absorbing large amounts of water or biological fluids. Due to their high water content, porosity & soft consistency, they closely simulate natural living tissues, more so than any other class of synthetic biomaterials. Hydrogels can be formulated in a variety of physical forms, including slabs, micro-particles, Nano-particles, coatings and films. As a result, hydrogels are commonly used in clinical practice & medicine for a wide range of applications, including Tissue engineering & Regenerative medicine, Diagnostics, Cellular immobilization, separation of biomolecules or cells, & barrier materials to regulate biological adhesions. Hydrogels are also relatively deformable & can conform to the shape of the surface to which they are applied. In the latter context, the bioadhesive properties of some hydrogels can be advantageous in immobilizing them at the site of application or in applying them on surfaces that aren’t horizontal. They have started to create a niche in several fields of medicine like in specific site drug delivery, tissue reconstruction & tissue engineering and even as biosensors. In this review article an attempt has been made to explain the properties of hydrogels, their methods of preparation & its applications.

Keywords: Hydrogel Properties, Classification, Technologies adopted, Applications

ABSTRACT

The objective of this study was to determine the efficacy of Plumbagin on attenuating malondialdehyde (MDA) and nitric oxide (NO), along with augmenting the endogenous antioxidant status in DMBA induced mammary carcinoma. Breast cancer was induced by providing 1ml of 7, 12 dimethyl benze (a) anthrecene(DMBA) 20mg/kg of body weight through orally and tissue antioxidants status along with histopathological studies were determined as per standard procedures. Western blot was also analyzed to determine the protein expression in all the experimental groups. Altered antioxidant status and upsurge free radical generation especially nitric oxide was observed in DMBA induce group when compared to control. This increase NO level was well supported by increase protein expression of iNOS and eNOS. However the altered antioxidant status was corroborated with decrease GSH protein expression. To support the detrimental effect of DMBA histopathology study showed neovasularization, presence of uniformly malignant ductal epithelial cells growing in vague cribiform pattern, necrosis formation along the tumor, and cell destructions. However, Plumbagin when administered at 4 mg/kg body weight showed attenuated free radical generation and upregulated the antioxidant activity. The increase free radical generation especially NO is also plays a pivotal causative role in breast cancer. Therapeutic efficacy targeting the antioxidant system could play a pivotal role in the treatment of breast cancer.

Keywords:7, 12 dimethyl benze (a) anthrecene (DMBA), Nitric oxide (NO), Nitric oxide synthase (NOS), Plumbagin, Antioxidant and Breast cancer

ABSTRACT

A selective, robust, economic and short method was developed for the simultaneous estimation of the Ertugliflozin (EGZ) and Sitagliptin (SGP) in Tablet dosage form. Chromatogram was run through  X-bridge c18 50 x 2.1 mm, 1.7m. Mobile phase containing Buffer: Acetonitrile taken in the ratio 50:50 was pumped through column at a flow rate of 1 ml/min. Buffer used in this method was 0.01N KH₂PO₄(3.0PH)buffer. Temperature was maintained at 30°C. Optimized wavelength selected was 240 nm Retention time of EGZ and SGP were found to be 0.883 min and 1.465 min. %RSD of the EGZ and SGP were and found to be 0.3 and 0.8 respectively. %Recovery was obtained as 99.83% and 100.09% for EGZ and SGP respectively. LOD, LOQ values obtained from regression equations of EGZ and SGP were 0.139, 0.421 and 0.18, 0.56 respectively. Regression equation of EGZ is y = 4300x + 253.6, and y = 6814x + 11844 of SGP. Retention times were decreased and that run time was decreased, so the method developed was simple and economical that can be adopted in regular Quality control test in Industries

Keywords: Ertugliflozin, Sitagliptin, UPLC.

ABSTRACT

3D-Quantitative structure metabolism relationship studies were conducted on the substrates of CYP3A4 based on CoMFA. The CoMFA model was found to be successful in the prediction of catalytic activity of CYP3A4 substrates, with a cross-validated correlation co-efficient (q²) of 0.593 and a non-cross validated correlation co-efficient (r²) of 0.994. The CoMFA model was also validated with the training and test set of CYP3A4 substrates. The model helped to understand the structural features that are involved in CYP3A4 mediated drug metabolism. Therefore, the model can be subjected to the initial stage of the drug discovery processes for developing the therapeutic analogs with the improved CYP3A4 mediated metabolic profiles.

Keywords: 3D-QSMR, CoMFA, Drug metabolism, CYP3A4

ABSTRACT

Alpha amylase is one of the important targets in the treatment of diabetes mellitus that work by preventing the digestion of carbohydrates. Many alpha amylase inhibitors with diverse chemical structures and modes of protein interaction have been designed on the basis of their ability to compete with alpha amylase enzyme. This study involves the molecular docking of certain novel isoxazole incorporated coumarin derivatives as potent alpha amylase inhibitory agents. The compounds were computationally designed and optimized with the docking to investigate the interactions between the target compounds and the amino acid residues of theα-amylase enzyme. The inhibitory activities against human alpha amylase enzyme were investigated by molecular docking using the autodock software. All the designed compounds were showed good binding energy when compared with the binging energies of standard drugs such as acarbose (for anti-diabetic activity). Among all the designed compounds, compoundI1 and I3 have more binding energy values when compared with standard drugs. Here we also studied the molecular properties of designed compound using molinspiration software. Further we planned to synthesis these isoxazole derivatives and screen for in vitroanti diabetic activity.

Keyword: Alpha amylase, isoxazole derivatives, docking, autodoc

ABSTRACT

Medicinal herbs as potential source of therapeutics have marked a crucial role in health system globally for both humans and animals. These are not only beneficial in the diseased condition but also used as potential material for maintaining proper health. The present study highlights the pharmacognostic studies on roots like powder microscopy and anthelmintic activity of different extracts on Indian adult earthworms. Different concentrations (50-150 mg/ml) of plant extract were tested in this study. Albendazole (20 mg/ml) was used as reference standard drug whereas CMC as control. Determination of paralysis time and death time of the worms were recorded. Extract exhibited significant vermicide activity in dose dependent manner. The result shows that methanolic extract possesses anthelmintic activity and found to be effective as an anthelmintic.

Keywords: Roots, Microscopy, In-vitro, Anthelmintic, Spanish pellitory, Fetida

ABSTRACT

Solid lipid nanoparticles (SLNs) are very potential formulations for topical delivery of antifungal drugs. The main objective for this investigation is to develop and optimize the SLNs of Acitretin for the effective topical delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultra sonication using Taguchi’s design and based on the results further investigation was made using central composite design (CCD). The lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, TEM, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. In vitro drug release of optimized SLN formulation (F2) was found to be 95.63±1.52%, whereas pure drug release was 30.12 after 60 min. The optimized formulation was incorporated into the gel. The drug content of Acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 10³± 0.4 x 10³ cp. The release rate (flux) of Acitretin across the membrane and excised skin differs significantly. It is assumed that SLN based gel due to its appropriate physicochemical properties, high skin permeation ability, higher accumulative uptake in skin and improved skin tolerability may be more suitable as a novel regime for topical administration of Acitretin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis with minimal drug systemic availability and high skin tolerability.

Keywords: Acitretin, Psoriasis, topical gel, skin permeation, histopathological studies

ABSTRACT

Lornoxicam is a non steroidal anti-inflammatory drug (NSAID) of the oxicam class. It belongs to BCS class II substance with low solubility and high permeability. The aim of current research is to formulate solid dispersion incorporated Fast disintegrating tablets of Lornoxicam to enhance the dissolution rate and aqueous solubility and to enable faster onset of action. Solid dispersions are prepared with polymers like Kolliwax GMS, Soluplus and HPMC in three different ratios 1:1:1, 1:2:1 and 1:3:1. Formulations were characterized for drug content studies, drug release studies and drug-polymer interactions using Fourier transform infrared spectroscopy (FTIR) spectrum. The solid dispersions can be evaluated by in-vitro dissolution studies. The optimized solid dispersion SD9 was further used to prepare fast disintegrating tablet by direct compression method using 3³ Response surface method (3 variables and 3 levels of superdisintegrants) by using Design of experiment software with superdisintegrants like locust bean gum, gum karaya, Plant ago ovata. The values of pre-compression parameters evaluated were within prescribed limits that indicated good free flowing properties. The data obtained of post-compression parameters such as weight variation, hardness, friability, content uniformity, disintegration time (33 sec) and percentage drug release was maximum in LF24(99.21±1.87%) and was found to superior over conventional formulation. It can be concluded that fast disintegrating tablets using Lornoxicam solid dispersion could be used to improve better patient compliance in the effective management of pain and inflammation.

Keywords: Lornoxicam, NSAID’s, Solid dispersion, fast disintegrating tablets, Response surface methodology.

ABSTRACT

Bortezomib is formulated as the solid lipid nanoparticle (SLN) system with the use of a 3-factor, 3-level Box–Behnken design, by hot homogenization followed by an ultra sonication method. Trimyristin (Dynasan-114), tripalmitin (Dynasan116) and tristearin (Dynasan-118) were used as lipids and based on the results from the initial studies tripalmitin (Dynasan116) was selected as the lipid for the further studies along with phosphate dylcholine as surfactant and Poloxamer 188 as stabilizer. The optimized formulation (F1) was obtained with minimum particle size (204 nm), maximum entrapment efficiency (70.24) and drug loading (21.24). In vitro release studies showed that maximum cumulative drug release was obtained for F1 (99.74%). The optimized formulation Bortezomib followed zero-order release kinetics with a strong correlation coefficient (R²= 0.9994). The pharmacokinetic studies in rabbits demonstrated that SLN formulation could be used for increasing the oral bioavailability of the drug for more than 2 fold when compared with pure drug. SLNs of Bortezomib were successfully developed to yield an optimized formulation with lowest particle size and highest entrapment efficiency that could sustain the release of drug.

Key words: Bortezomib, SLN, Cancer, Tripalmitin, Box-Behnken design, Pharmacokinetic studies.

ABSTRACT

Murraya koenigi is a medium sized tree belonging to the family Rutaceae. The major constituents present in the Murraya koenigii leaves treat burns, bruises. Ayurveda is a traditional Indian medicinal system practiced for thousands of years. Natural remedies are more acceptable in the faith that they are safer with less side effects than the synthetic ones. The novel formulations are reported to have remarkable advantages over conventional formulations of plant actives and extracts which include enhancement of solubility, bioavailability, protection from toxicity, enhancement of pharmacological activity, enhancement of stability, improved tissue macrophages distribution, sustained delivery and protection from physical and chemical degradation. Our main purpose is to treat/heal wound at faster rate with minimum side effects. Nanosponges alone are difficult to use on local tissues because they diffuse away to other parts of the body very quickly so to overcome the drawback we combined nanosponges with the herbal extract of Murraya Koenigii. According to literature survey it was found that etanolic and aqueous extract shows good wound healing results. Research on curry leaves revealed that they are also effective in fighting bacterial and fungal infections. The leaf extracts from the plant have been comparable to popular main stream antibiotic drugs. During this research work, we prepared ethanolic extract of Murraya Koenigii leaves and prepared nanosponges from it for treating burn wound. The nanosponges are prepared by Quasi emulsion solvent diffusion method. The prepared nanosponges were evaluated for various in-vitro parameters and the results obtained were satisfactory.

Keywords: Nanosponges, Murraya koenigii, wound, solubility

ABSTRACT

A new, simple, rapid, selective, precise and accurate isocratic reverse phase high performance liquid Chromatography assay method has been developed for simultaneous estimation of Isoniazid and Pyridoxine tablet formulations. The separation was achieved by using column Hypersil BDS, (250 x 4.6 mm, 5 µ) (Make: Thermo), in mobile phase consisted of pH4.0 phosphate buffer and Acetonitrile in the ratio of 75:25 v/v. The flow rate was 1.0 mL/min, column oven temperature 30° C, the injection volume was 10 μL, and detection was performed at 267 nm using a photodiode array detector (PDA), Run time 6 minutes. The retention time of Isoniazid and Pyridoxine, was noted to be 3.5 minutes and 4.3 minutes respectively, indicative of rather shorter analysis time. The method was validated as per ICH guidelines. The proposed method was found to be accurate, reproducible, and consistent.

Keywords: Liquid Chromatography; Isoniazid, Pyridoxine, combined dosage forms; Simultaneous estimation, Validation

ABSTRACT

Stem cell therapy is the use of Stem cells to treat or prevent disease or condition. Stem cell therapy is emerging as potent new way to treat disease and injury with wide range medical benefits. Research is underway to develop various sources for stem cells and to apply stem cell treatment for neurodegenerative diseases and conditions diabetes, heart diseases and other conditions. However stem cells therapy produce many ethical and scientific questions that are to be solved. Nevertheless, stem cells therapy, a preamble to research of cell based therapeutics, will one day restore the functionality of the formerly un abled people, is yet to be unvealed.

Keywords: SC- stem cell, MSCs- multi potent mesenchymal stromal cells, ES cells- embryonic stem cells, HIV -human immunodeficiency virus type-1.

ABSTRACT

In order to gather all the information concerning the nature and the therapeutic uses of the medicinal plants, an ethnobotanical study of the medicinal plants was realized Oran city’s circle, between December 2017 and April 2018. This research was conducted in collaboration with different plant users such as ordinary users (500 people) who were randomly selected (340 women, 160 men). The survey targeted 500 people from the local population, including 423 people preferring medicinal plants with a rate of 84% and 77 people who received treatment in modern medicine with a rate of 16%. The results obtained from the population made it possible to identify 58 medicinal plants which are divided into 34 families, of which three are the most dominant, in particular Lamiaceae (29.55%), Apiaceae (17.96%) and Verbenaceae (14.65%). all listed plants with properties against allergy. the leaves are the most used organs (34%) and the majority of the remedies is prepared as an infusion (58%), the respiratory diseases occupy the first place with a rate of 42%. The results obtained constitute a very valuable source of information for the region studied and for the national medicinal flora. They could be a database for further research in the fields of photochemistry and pharmacology and for the purpose of searching for new natural substances.

Keywords: ethnobotany, medicinal plants, allergy, Oran, questionnaire, phyto therapy

ABSTRACT

Heart Failure (HF) is a complex clinical syndrome that can result from any structural or functional cardiac disorder that impairs the ability of the ventricle to fill with or eject blood. This is further subdivided into HF with reduced left ventricular ejection fraction (HFrEF) or HF with preserved left ventricular ejection fraction (HFpEF) previously known as diastolic HF. HF may be caused by disease of the myocardium, pericardium, endocardium, heart valves, vessels, or by metabolic disorders. Most patients with HFrEF should be routinely treated with guideline directed medical therapy (GDMT) that includes an angiotensin-converting enzyme (ACE) inhibitor or angiotensin receptor blocker (ARB) and a ?-blocker. Selected patients should also receive loop diuretics, hydralazine/nitrates, or aldosterone antagonists. The benefits of these medications on slowing HF progression, reducing morbidity and mortality, and/or improving symptoms are clearly established, Digoxin is potentially beneficial in symptomatic patients with HFrEF already receiving optimal medical therapy to decrease HF hospitalizations. There is little clinical trial evidence to guide which treatment are optimal to use in HFrEF.

Keywords: Heart Failure, Angiotensin-converting enzyme.

ABSTRACT

In the era of increasing demand for indigenous medicines, maintaining quality standards is the need of the hour. Standardisation of compound formulations is lagging behind because of absence of reference standards. Manjishthadi Ghanavati is an important Ayurvedic formulation containing Manjishtha (Rubia cordifolia Linn.), Haritaki (Terminalia chebula Retz.), Amalaki (Emblica officinalis Gaertn.), Bibhitaki (Terminalia bellerica Roxb.), Katuki (Picrohriza kurroa Royle. ex Benth), Vacha (Acorus calamus Linn.), Daruharidra (Barberis aristata DC) Guduchi (Tinospora cordifolia Willd.) and Nimba (Azadirechta indica A Juss.). All the constituents are available and prepared according to the reference present in Sharangadhara Samhita Madhyama Khanda Chapter 2/136. Hence the present study was undertaken to standardize the compound Ayurvedic formulation through Pharmacognostical and pharmaceutical evaluation. The sample was subjected for various phytochemical parameters like water soluble extractive (49.72%w/w), alcohol soluble extractive (41.28 % w/w), ash value (10 % w/w), loss on drying (10.85 % w/w), the pH (6.0), Hardness(4 kg/cm²⁾ and Disintegration time (32 min.). The HPTLC, solvent system was Toluene: ethyl acetate (9:1), showed the presence of 7 spots at 254nm and 2 spots at 366nm. Thus, the physiochemical and microscopic characters achieved may provide guidelines for standardization of formulation Manjishthadi Ghanavati.

Keywords: HPTLC, Manjishthadi Ghanavati, Pharmacognostical, Physiochemical Evaluation.

ABSTRACT

The purpose of this research was to prepare and evaluate a floating drug delivery system of a proton pump inhibitor (pantoprazole sodium). Pantoprazole is a proton pump inhibitor, belongs to group of benzimidazole, used for the treatment of gastric and duodenum ulcers. The core tablets were prepared by direct compression method (effervescent method) by using microcrystalline cellulose, sodium bicarbonate, citric acid, magnesium stearate and HPMC K100 and HPMC K15. The physicochemical parameters like pre-compression and post compression evaluation were performed as per Pharmacopoeial standard and the compatibility study was performed by FTIR and DSC methods. The release data were subjected to different models in order to evaluate their release kinetics and mechanisms. The compatibility study of the prepared Pantoprazole sodium tablets implies the information about no interaction between drug and polymer. The drug release kinetics was observed by Non-Fickian diffusion mechanism. HPMC K100 shows better release properties than HPMC K15. The floating lag time were found to be significantly increased with the increasing concentration of the gas generating agent. After the dissolution study of prepared Pantoprazole sodium floating tablet, it was concluded that the formulations with HPMC K100 shows better controlled release effect than HPMC K15. The release kinetics data implies that the release mechanism of the all formulation was Non-Fickian. The developed floating tablets of pantoprazole sodium may be used in clinic for prolonged drug release for at least 12h, thereby improving the bioavailability and patient compliance.

Keywords: Pantoprazole sodium, Gastro retentive, Floating drug delivery systems, Release kinetics. Buoyancy studies.

ABSTRACT

In present investigation the anticancer properties of Boerhaavia diffusa were studied. Carcinogenicity was induced by DEN i.e. nitrosamine (@ 200 µl/Kg body weight). In a single dose DEN challenged animals were given Boerhaavia diffusa extract (@200mg/Kg body weight) daily and named them as test group. For control group no DEN and no treatment was given. Negative control was given only DEN, to check its carcinogenicity with control and test group. After eight weeks the blood samples were collected to study the effect of carcinogen and plant extract of Boerhaavia diffusa. Various biochemical parameters like : Superoxide dismutase (SOD), Glutathione (GH), Alkaline phosphatase (ALP), Acid phosphatase (ACP), SGOT, SGPT, Triglycerides, Albumin, Catalase (CAT), Lipid per oxidation (MDA), Total proteins (TP), Globulin, Albumin-Globulin ration, Bilirubin, Creatinine, Total cholesterol, HDL, LDL, HDL/LDL ratio and body weight gain were studied. The results of the present study showed that there was a significant decrease in body weight gain among all the groups. Significant increase in SOD, MDA, GH, ALP, ACP, SGPT, SGOT etc. and CAT, TP, Albumin, Globulin, Total Cholesterol, HDL, Triglycerides were significantly decreased as compared with control group. The test group had shown significant hepato protective and anti carcinogenic activity against DEN. The biochemical changes were also supported by histopathological lesions. The present study concludes that plant extract of Boerhaavia diffusa have shown hepato protective and anti liver cancer activity.

Keywords: Anticancer, Hepatoprotective, Diethyl nitrosamine, Boerhaavia diffusa, biochemical parameters and histopathology.

ABSTRACT

The current work is carried out to for estimation of Chlorcyclizine Hydrochloridein bulk by utilizing area under curve (AUC) method using UV-Visible spectrophotometry. For this purpose the wavelength range 220-240nm was selected. Distilled water was used as a solvent throughout the work. Linearity was observed in concentration range 5-25µg/ml (R²=0.996) for the method. The present method was found to be simple & linear which can be used for routine quality control analysis for spectrophotometric estimation of Chlorcyclizine Hydrochloride in bulk.

Keywords: Chlorcyclizine Hydrochloride, Area under curve, Antihistaminic, λmax.

ABSTRACT

Present investigation was done for screening microorganism with highly stable xylanase production. In present days, commercial microbial enzymes are increasingly replacing conventional chemical catalysts in many industrial processes. In current studies 56 actinomycetes were found positive for xylan-degradation. Among all isolates, best actinobacter found for xylanase production was rare species and less identified for any such properties. During studies Microbacterium hatanonis HAX-5 was found potential for xylanase production in submerged fermentation using agrowaste.

Keywords: Xylanase, Microbacterium hatanonis HAX-5, Submerged Fermentation