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Current Trends in Biotechnology and PharmacyVol. 5 (2) 1104-1109 April 2011. ISSN 0973-8916 (Print), 2230-7303 (Online)1109modern drug discovery research: the Rocheexperience. Drug Discovery Today, 11:326-333.9. Dessalew, N. and Singh S.K. (2008). 3D-QSAR CoMFA and CoMSIA study onBenzodipyrazoles as Cyclin DependentKinase 2 Inhibitors. Medicinal Chemistry. 4:313-321.10. Lu, X.Y., Chen, Y.D., Sun, N.Y., Jiang, Y.J.and You, Q.D. (2010). Molecular-dockingguided3D-QSAR studies of substitutedisoquinoline-1,3-(2H,4H)-diones as cyclindependentkinase 4 (CDK4) inhibitors.Journal of Molecular Modeling. 16: 163-173.11. Herve, F., Caron, G., Duche, J-C., Gaillard,P., Abd Rahman, N., Tsantili-Kakoulidou, A.,Carrupt, P.A., Dathis, P., Tillement, J.P. andTesta, B. (1998). Ligand Specificity of theGenetic Variants of Human α1-AcidGlycoprotein: Generation of a Three-Dimensional Quantitative Structure-ActivityRelationship Model for Drug Binding to theA Variant. Molecular Pharmacology. 54: 129-138.12. Gianazza, L., Eberini, I., Villa, P., Fratelli, M.,Pinna, C., Wait, R., Gemeiner, M. and Miller,I. (2002). Monitoring the effects of drugtreatment in rat models of disease by serumprotein analysis. Journal of ChromatographyB: Analytical Technologies in the Biomedicaland Life Sciences, 771: 107-130.13. Singh, S.K., Dessalew, N and Bharatam, P.V.(2006). 3D-QSAR CoMFA study onindenopyrazole derivatives as cyclindependent kinase 4 (CDK4) and cyclindependent kinase 2 (CDK2) inhibitors.European Journal of Medicinal Chemistry, 41:1310-1319.14. Kulkarni, R.G., Srivani, P., Achaiah G. andSastry, G. N. (2007). Strategies to designpyrazolyl urea derivatives for p38 kinaseinhibition: a molecular modeling study. Journalof Computer-Aided Molecular Design, 21(4):155-166.15. Chung, J.Y., Chung, H. W., Cho, S. J., Hah,J.M. and Cho, A. E. (2010). QM/MM based3D QSAR models for potent B-Raf inhibitors.Journal of Computer-Aided MolecularDesign, 24(5): 385-397.16. Goodman, D., Morrison, M. (2004) JavaScript Bible (6 th edition), John Wiley, USA.17. Powell, T.A and Schneider, F. (2004)JavaScript: the complete reference (2 ndedition), McGraw-Hill, USA.18. Tamaoki, T., Nomoto, H., Takahashi, I., Kato,Y., Morimoto, M. and Tomita, F. (1986).Staurosporine, a potent inhibitor ofphospholipid/Ca ++ dependent protein kinase.Biochemical and Biophysical ResearchCommunications, 135: 397-402.19. Dessalew, N., Bharatam, P. and Singh, S.K.(2007), 3D-QSAR CoMFA Study onAminothiazole Derivatives as Cyclin-Dependent Kinase 2 Inhibitors. QSAR &Combinatorial Science, 26: 85–91.20. Raj, N. Misra., Hai-yun. Xiao., Kyoung. S.Kim., Songfeng. Lu., Wen-Ching. Han.,Stephanie. A. Barbosa., John. T. Hunt., David.B. Rawlins., Weifang. Shan., Syed. Z.Ahmed., Ligang. Qian., Bang-Chi. Chen.,Rulin. Zhao., Mark. S. Bednarz., Kristen. A.Kellar., Janet. G. Mulheron., RobertaBatorsky., Urvashi. Roongta., Amrita.Kamath., Punit. Marathe., Sunanda. A.Ranadive., John. S. Sack., John. S. Tokarski.,Nikola. P. Pavletich., Francis. Y. F. Lee.,Kevin. R. Webster and S. David. Kimball.(2002). N-(Cycloalkylamino)acyl-2-aminothiazole Inhibitors of Cyclin-DependentKinase 2. N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-piperidinecarboxamide (BMS-387032), aHighly Efficacious and Selective AntitumorAgent. J. Med. Chem. 47, 1719-1728.Chandrabose Selvaraj et al
Current Trends in Biotechnology and PharmacyVol. 5 (2) 1110-1122 April 2011. ISSN 0973-8916 (Print), 2230-7303 (Online)Formulation, Characterization and Pharmacokinetic Studies ofCarvedilol NanoemulsionsKoteswari Poluri 1 , Ramakrishna Sistla 2 , Prabhakar Reddy Veerareddy *3 ,Lakshmi M. Narasu 4 , Amol A Raje 5 and Sunder M. Hebsiba 51S. N. Vanitha Pharmacy Maha Vidyalaya, Nampally Exhibition Grounds, Hyderabad, A.P, India2Indian Institute of Chemical Technology, Tarnaka, Hyderabad, A.P, India3St. Peter’s Institute of Pharmaceutical Sciences, Hanamkonda, Warangal, A.P, India4Centre for Biotechnoloy, Jawaharlal Nehru Technological Unviersity, Hyderabad, A.P, India5Vimta labs Ltd., 5, S.P.Biotech Park, Shameerpet, Hyderabad, A.P, India*For Correspondence - vpreddyindia@yahoo.com1110AbstractThe present study involves the formulationand evaluation of oral o/w nanoemulsions (NE)with two simple edible oils, avoiding the largequantities of surfactants and co-surfactants whichwere prepared by high energy emulsificationtechnique. The particle size, polydispersity index(PDI), and zeta potential of prepared nanoemulsions were determined by using zeta sizerand were found to be in the range of 33.4±3.9nm, to 183.56±1.78nm, 0.051±0.04 to 0.38±0.06and -2.87±0.65 to -14.2±0.72 mv respectively.Centrifugation, freeze-thaw cycling, storage at4°C for 60days, X-ray diffraction (XRD) andTransmission electron microscopy (TEM) studiesrevealed the physical and chemical stability ofthe NEs. Entrapment efficiency and in-vitrorelease studies showed successful incorporationof carvedilol into NE with high drug loadingefficiency and good stability. Comparativepharmacokinetic studies of NE and marketeddosage form in male SD rats revealed a significantincrease in oral bio availability in NEs.Key words: Nano emulsions, Sesame oil, Oliveoil, Carvedilol, Sonication, LC-MS/MSIntroductionNano technology has emerged as one ofthe very promising fields of biomedical researchin the last few decades. Nano technology basedhealth care products will expected to reach 2trillion dollars target by the year 2015(1). Nanoemulsion technology is one of the segments ofnano technology market and can be defined asthermodynamically stable, transparent ortranslucent dispersions of oil and water having asize range of 50-200 nm (2).Different types of oils and components canbe used for the preparation of NEs to impartspecific properties such as crossing different typesof biological barriers like blood brain barrier uponadministration (3). NEs can also be used asexcellent vehicles in pharmaceutical field for theparenteral, oral and ocular or transdermal deliveryof poorly permeable lipophilic drugs. Because ofthese unique properties, nano emulsions aregaining more importance as potential vehicles forthe efficient delivery of lipophilic drug molecules(3, 4, 5).Cardiovascular diseases includinghypertension are one of the major causes ofmortality in the world. Delivery of therapeuticagents to cardiac organelles has the potential toincrease the efficiency of treatment protocols forheart failure. However, cardiac cells presentspecial problems to the delivery of drugs, and thenumber of papers reported in this area is also avery few (6). Carvedilol was selected for thepresent study. It is a non selective beta adrenergicFormulation, characterization and Pharmacokinetic studies
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(December 7-9, 2011)Venue: Karunya
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