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Development of Tri Block Copolymer Micelles to Enhance Solubility of Poorly Water Soluble Drug: By Response Surface Methodology

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The aim of the present study was to formulate and evaluate polymeric micelles (PMs) for enhancing the solubility of a BCS Class II drug. The PMs of the model drug, carbamazepine (CBZ) were prepared using Pluronic F127 by solvent evaporation method. 23 Factorial design was selected for the preparation of the formulations. Independent variables selected were temperature, concentration of the drug and the polymer and dependent variables selected were % drug released in the first hour (Y1) and % encapsulation efficiency (Y2). The quantitative effect of the independent variables at different levels on dependent variables was predicted using polynomial equations. The prepared polymeric micelles were characterized using FTIR, DSC, SEM, zeta potential and were evaluated for particle size, encapsulation efficiency, in vitro drug release. FTIR and DSC studies showed compatibility between the drug and the polymer. The particle size and zeta potential of prepared formulations were found to be between 186 to 892 nm and –12.4 to –26.7 mV respectively. Drug loading and Encapsulation efficiency for the prepared formulations were found to be in the range of 16.4 to 19.6% and 32.1 to 42.7% respectively. In vitro drug release of the prepared formulations was done in pH 1.2 buffer for 60 min and the release was found to be between 80.99% to 100.9%. The oral bioavailability of CBZ from these self-assemblies revealed 85% and 5% increase versus CBZ coarse suspension and Carbatrol® respectively. Hence it can be concluded that the PMs prepared seem to be promising carriers for enhancing the solubility of poorly water soluble drug.
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Keywords: BIOAVAILABILITY STUDIES; CARBAMAZEPINE; FACTORIAL DESIGN; IN VIVO; PLURONIC F-127; POLYMERIC MICELLES

Document Type: Research Article

Publication date: August 1, 2015

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  • Advanced Science, Engineering and Medicine (ASEM) is a science, engineering, technical and medical journal focused on the publishing of peer-reviewed multi-disciplinary research articles dealing with all fundamental and applied research aspects in the areas of (1) Physical Sciences, (2) Engineering, (3) Biological Sciences/Health Sciences, (4) Medicine, (5) Computer and Information Sciences, (6) Mathematical Sciences, (7) Agriculture Science and Engineering, (8) Geosciences, and (9) Energy/Fuels/Environmental/Green Science and Engineering.
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