Original Articles: 2015 Vol: 7 Issue: 2
Formulation and in vitro characterization of Carbamazepine polymeric nanoparticles with enhanced solubility and sustained release for the treatment of Epilepsy
Abstract
Carbamazepine is used in the treatment of epilepsy, but it is having limitations such as low solubility leading to lower oral bioavailability. Carbamazepine conventional formulation despite having good anti epileptic activity, its therapeutic activity was limited due to its slow and limited release in gastrointestinal tract. So the major objective was to formulate polymeric nanoparticles, which can increase solubility and drug release along with sustained release property of the drug. In the present study, it was proposed to develop nanotechnology-based systems, for selected poorly water-soluble drug carbamazepine using PLGA as polymer (with different drug: polymer ratios) selected randomly by factorial method designing and was expected to improve dissolution properties that may increase its bioavailability. The polymeric nanoparticles were subjected to particle size evaluation, SEM study, drug content, entrapment efficiency and in vitro release studies. Nanoparticles with drug: polymer ratio of 1:1 has shown a particle size, drug loading and entrapment efficiency of 130±2.1nm, 61.28% and 18.15 % respectively. Optimized batch in drug: polymer ratio of 1:1 has shown a particle size, drug loading and entrapment efficiency of 126.8±0.19m, 34.81±0.01% and 64.28±0.09% respectively. Contour plots and 3D-scatter plots were drawn for statistical supportive evaluation in optimization using Minitab 17. In vitro drug release studies concluded that carbamazepine nanoparticles released drug in biphasic pattern by initial burst release of 50±0.12% with in 4 hours, which was followed by sustained release of 89.92±0.01% till 24 hours concluding its solubility enhancement.