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Setty C.M.,Vishnu Institute of Pharmaceutical Education and Research | Deshmukh A.S.,Shree Dhanvantary Pharmacy College | Badiger A.M.,BDR Pharmaceuticals International Private Ltd
International Journal of Biological Macromolecules

The present study investigates the pharmaceutical application of hydrolyzed polyacrylamide grafted carboxymethylxyloglucan (HPam-g-CMXG), as promising polymeric material for the development of pH responsive microbeads. The graft copolymer was synthesized by conventional free radical polymerization method and saponified to enhance its functionality and characterized. An acute oral toxicity study ensured the bio-safety of developed copolymer for clinical application. Various batches of pH responsive spherical microbeads were developed and evaluated for the effect of process parameters on their overall performance. Result of in vitro drug release study (USP Type-II, paddle method) carried out in two different pH media (pH 1.2 and pH 7.4) showed a triphasic drug release pattern in all the formulations. Both the drug release and swelling of microbeads were significantly higher in simulated intestinal (alkaline) pH compared to simulated gastric (acidic) pH and this nature is desirable for targeted drug delivery. A strong correlation was observed between the process parameters and matrix composition and it directly influenced the drug transport mechanism. In conclusion, the hydrolyzed polyacrylamide grafted carboxymethylxyloglucan holds an immense potential to be explored pharmaceutically as new matrix material for the design of targeted drug delivery system. © 2014 Elsevier B.V. Source

Mukkanti K.,JNTUH College of Engineering | Deepak Reddy G.,Vishnu Institute of Pharmaceutical Education and Research
Tropical Journal of Pharmaceutical Research

Purpose: To synthesize Schiff bases of 2-aminothiophenes and evaluate their anticonvulsant activity and in silco properties Methods: 2-Amino-N-o-tolyl-5,6-dihydro-4H-cylcopenta[b]thiophene-3-carboxamide was synthesized using 1,1,3,3-tetramethylguanidine lactate as a basic catalyst and by microwave irradiation. 2- substitued-o-tolyl-5,6-dihyro-4H-cylcopenta[b]thiophene-3-carboxamide was prepared by reacting with different substituted aromatic aldehydes. The synthesized compounds were characterized by Fourier transform infrared spectroscopy (FTIR), nuclear magnetic resonance spectroscopy (1H NMR) and mass spectrometry (MS) while their anticonvulsant activity was screened against maximum electroshockinduced seizure (MES), and pentylenetetrazole-induced seizure (PTZ) against phenytoin and diazepam as reference standards. Molecular docking (in silico) studies were performed using 4-aminobutyrateaminotransferase in order to predict possible protein-ligand interactions. Results: Among the 21 synthesized compounds, 2b, 2d, 2f, 2k, 2m, 2n and 2o showed good to moderate activity against MES and PTZ-induced convulsions. Compounds 2b, 2d, 2f, 2k and 2m exhibited lower activity against PTZ than against MES model while compounds 2n and 2o afforded greater protection against PTZ than against MES model. In silico results also revealed maximum binding affinity to GABA-AT protein which was higher than other compounds Conclusion: The synthesized compounds showed potent anticonvulsant activity. Molecular docking results should give an insight into how further modification of lead compound can be carried out for higher inhibitory activity. © Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, 300001 Nigeria. Source

Babu Y.R.,Gland Institute of Pharmaceutical science | Bhagavanraju M.,Gland Institute of Pharmaceutical science | Reddy G.D.,Vishnu Institute of Pharmaceutical Education and Research | Peters G.J.,VU University Amsterdam | And 2 more authors.
Archiv der Pharmazie

In a quest for finding potent cytotoxic molecules, we have designed and synthesized a new scaffold by tagging quinazolinones with an acridone moiety. The new acridone-4-carboximide derivatives were evaluated for their cytotoxic potentials against the MCF7 breast cancer cell line and three colon cancer cell lines (LS174T, SW1398, and WiDr). Compound 26 showed relatively potent cytotoxic activity among the derivatives, against all the cell lines tested. Mechanistic studies for the selected derivatives 7, 8, 16, 17, 25, and 26 were conducted through in vitro EGFR tyrosine kinase inhibition studies. The results indicate that compound 26 has a better EGFR tyrosine kinase inhibitory profile. The in vitro EGFR inhibition data was correlated with the cytotoxic properties, and molecular docking studies were performed with regard to the receptor autophosphorylation sites of the protein kinase domain of the EGFR. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. Source

Kalshetti P.B.,Maharashtra Institute of Pharmacy | Alluri R.,Vishnu Institute of Pharmaceutical Education and Research | Thakurdesai P.A.,Indus Biotech Private Ltd
Brazilian Archives of Biology and Technology

The objective of this work was to evaluate the effects of standardized hydroalcholic extract of Commiphora mukul (HECM) in animal model of chronic stress medicated depression, namely olfactory bulbectomy (OBX) model in rats. Effects of 14-day (subacute) oral pretreatment of HECM (50, 100 and 200 mg/kg) were evaluated on depression and stress related parameters on OBX rats. Separate groups for sham control, OBX control and positive controls namely imipramine (20 mg/kg), fluoxetine (30 mg/kg) and desipramine (15 mg/kg) were also maintained. Behavioral and physiological parameters in open field and elevated plus maze were recorded. HECM showed dose-dependent reversal of OBX-induced physiological effects such as reduction of body weight, body temperature, heart rate and serum sodium concentration. HECM also showed reversal effects on OBX induced food intake increase and hyperactivity in open field and elevated plus maze paradigm. In conclusion, HECM demonstrated restorative effects in OBX induced depression model in rats probably due to stress reliving mechanisms. Source

Mallikarjuna Setty C.,Vishnu Institute of Pharmaceutical Education and Research
Digest Journal of Nanomaterials and Biostructures

The aim of the present study was to develop and characterize nanoemulsion formulation of tamoxifen citrate (TAM) for transdermal drug delivery system. Various oil-in-water nanoemulsions were prepared by the aqueous titration method. The prepared nanoemulsions were subjected to thermodynamic stability study and characterized for droplet size, transmission electron microscopy (TEM), viscosity studies. FTIR study was subjected to ensure the compatibility among its ingredients. Transdermal permeation of tamoxifen citrate through rat skin was determined by Keshary-Chien diffusion cell. Penetration enhancers effects on the skin permeation of TAM were investigated. Pharmacokinetic and pharmacodynamic parameter was determined on optimized formulations. Mean globule size and viscosity was found to be lowest in A1 formulation. TEM demonstrated spherical particle morphology and FTIR study revealed the compatibility among the ingredients. Significant increase in steady - state flux (Jss) was observed in optimized A1 and DA1 nanoemulsion. Of the various essential oils added, dill oil had the best enhancing ability. In pharmacokinetics study, transdermally applied nanoemulsion increased in bioavailability as compared to oral tablet formulation. In pharmacodynamic study RTV in mice receiving the optimized nanoemulsions was significantly reduced compared to control. Developed nanoemulsions can be used as potential vehicle for enhancement of bioavailability of TAM through transdermal application. Source

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