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Kankate R.S.,METs Institute of Pharmacy | Vanjari S.S.,Institute of Chemical Technology
International Journal of ChemTech Research

A series of 2'-hydroxychalcones and 3-hydroxyflavones were evaluated for in vitro antioxidant activity on four different models namely Diphenyl Picryl Hydrazine, Nitric Oxide, Hydrogen peroxide, and Phenyl hydrazine induced hemolysis of erythrocytes. The studies indicate that amongst evaluated 2'-hydroxychalcones, 2-Bromochalcone and 2-Chlorochalcones showed significant activity and amongst different 3-hydroxyflavone evaluated 3'-hydroxyflavones, 4'-methoxy and 4'-Chloroflavone showed significant activity. Source

Ahirrao S.,METs Institute of Pharmacy | Gide P.,METs Institute of Pharmacy | Shrivastav B.,Jaipur National University | Sharma P.,Jaipur National University
Particulate Science and Technology

Theophylline is the most useful bronchodilators for the treatment of severe reversible bronchospasm. The fluctuations of serum theophylline level in clinical practice and associated central nervous system side effects necessitate the development of an extended release formulation. In the present study, theophylline-loaded beads were prepared by extruding the dispersion of theophylline, sodium alginate, and glycerol into the cationic crosslinking solution of calcium chloride. The effect of the addition of glycerol was determined by entrapment efficiency, drug release, and morphology of beads. Absence of chemical interaction between drug, polymer, and counterions after production of beads was confirmed by Fourier transform infrared spectroscopy. Theophylline entrapment of up to 72% was achieved in beads with almost spherical shape and size ranging from 0.67 to 1.12 mm. Percentage entrapment of theophylline found to be more and release was extended up to the eleventh hour from the glycerol containing sodium alginate beads. Hence, sodium alginate glycerol beads could represent a promising oral drug delivery system to extend the release of theophylline. Copyright © 2014 Taylor & Francis Group, LLC. Source

Bedadurge A.B.,METs Institute of Pharmacy | Shaikh A.R.,METs Institute of Pharmacy
Journal of the Korean Chemical Society

Quantitative structure-activity relationship (QSAR) analysis for recently synthesized imidazole-(benz)azole and imidazole - piperazine derivatives was studied for their anticancer activities against breast (MCF-7) cell lines. The statistically significant 2D-QSAR models (r2 = 0.8901; q2 = 0.8130; F test = 36.4635; r2 se = 0.1696; q2 se = 0.12212; pred-r2 = 0.4229; pred-r2 se = 0.4606 and r 2 = 0.8763; q2 = 0.7617; F test = 31.8737; r2 se = 0.1951; q2 se = 0.2708; pred-r2 = 0.4386; pred-r 2 se = 0.3950) were developed using molecular design suite (VLifeMDS 4.2). The study was performed with 18 compounds (data set) using random selection and manual selection methods used for the division of the data set into training and test set. Multiple linear regression (MLR) methodology with stepwise (SW) forward-backward variable selection method was used for building the QSAR models. The results of the 2D-QSAR models were further compared with 3D-QSAR models generated by kNN-MFA, (k-Nearest Neighbor Molecular Field Analysis) investigating the substitutional requirements for the favorable anticancer activity. The results derived may be useful in further designing novel imidazole-(benz)azole and imidazole-piperazine derivatives against breast (MCF-7) cell lines prior to synthesis. Source

Nikumbh K.V.,METs Institute of Pharmacy | Sevankar S.G.,METs Institute of Pharmacy | Patil M.P.,METs Institute of Pharmacy
Drug Delivery

Background: Anti-inflammatory agents are widely used to relieve inflammation caused by various factors. Aim: This study was initiated with the intention to deliver low aqueous soluble ketoprofen to enhance its solubility by developing microemulsion system as a template and then incorporating it into gel phase. Materials and methods: Initially ketoprofen was solubilized into microemulsion preparation made up of clove oil, Tween 20 and propylene glycol as oil phase, surfactant and co-surfactant respectively, then it was incorporated into different concentration of gelling phase using gelling agents namely Carbopol 940, Carbopol 934 and hydroxypropyl methyl cellulose K4M (HPMC K4M). Formulated emulgels were evaluated for their physical appearance, pH, rheological properties, globule size, extrudability, drug content, spreadability, bioadhesion strength, in vitro and ex vivo drug release, skin irritation test and anti-inflammatory activity. Results: Microemulsion had shown globule size 396 nm, pH 6-6.7, viscosity 29.4 cps and zeta potential -12 mV indicating good stability. Formulated emulgels showed good physical appearance, skin acceptable pH 6-6.9, non-Newtonian shear thinning system, drug content 99.28 ± 0.16%, bioadhesion strength 48.4 gram force, globule size 473 nm, spreadability 22.96 gm.cm/s, good extrudability, in vitro release, ex vivo release did not showed any irritation reaction and possess a good anti-inflammatory activity. Conclusions: Selected batch showed enhanced drug release (92.42 ± 4.66%) as compared to marketed gel (65.94 ± 3.30). Similarly ex vivo release of formulation showed 72.22% release through mice skin compared with marketed gel. Formulations followed Korsmeyer-Peppas diffusion kinetic model. It was observed from the results that the formulated emulgel can provide promising delivery of ketoprofen. © 2013 Informa Healthcare USA, Inc. All rights reserved. Source

Patil S.D.,METs Institute of Pharmacy | Shelar K.E.,METs Institute of Pharmacy | Shakeel Z.H.,METs Institute of Pharmacy | Shaikh A.R.,METs Institute of Pharmacy
Der Pharma Chemica

Two dimensional quantitative structure activity relationship (2D-QSAR) and three dimensional quantitative structure activity relationship (3D-QSAR) studies by means of Multiple Linear Regression (MLR), Partial Least Square (PLS) and Principal Component Regression (PCR) were performed on a series of 4-Alkoxycarbonyl-1, 5-diaryl-1, 2, 3-triazole analogues for the treatment of drug abuse disorder using software MDS 4.2 version (VLife Science). This study was performed with 13 compounds (Data set) using random as well as manual data selection methods for the division of the data into training and test set. MLR methodology with stepwise (SW) forwardbackward variable selection method was used for building the QSAR models. Statistically significant QSAR models were generated. Among them most significant model has squared correlation coefficient (r2) = 0.9895, cross validated correlation coefficient (q2) = 0.9747 and predictive correlation coefficient (pred_r2) = 0.9826 for the treatment of drug abuse disorders. The core idea of the present study is the search for novel 4-Alkoxycarbonyl-1, 5-diaryl-1, 2, 3-triazole analogues that would show promise to be useful in the treatment of drug abuse disorders. Source

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