Formulation Characterization In Vitro and In Vivo evaluation of polymeric nanoparticles of tiagabine hydrochloride used in the treatment of epilepsy

Abstract

The aim of this research was to develop optimized bio compatible and bio degradable novel delivery systems of Tiagabine for effective treatment of epilepsy. PLGA and PEG-PLGA nanoparticles have the ability to control the drug release and the formulation avoids of the use of hazards organic solvents because of its solubility in acetic solution. Nanopaticles were prepared by Emulsion-Solvent Evaporation method. Cryoprotectant was added due to its protective effects in preventing particle aggregation during lyophilization. The particle size of nanoparticle controls the endocytosis rate across the brain capillary endothelial cells. For effective brain targeting of drugs, the size of the nanoparticles should be below 200 nanometer. The size of various batches of nanoparticles was found to vary between 130-300 nm and was optimized below 200 nm. PDI indicates size distribution of nanoparticles and lower value of PDI of all the batches indicates homogenous, unimodel, narrow particle distribution. Zeta potential values were observed and optimized. The high positive zeta potential value reflects strong repulsion lack of particle aggregation and the excellent physical stability. The average percentage of drug entrapment efficiency ranged from 65% to 85%. This study confirmed that the Emulsification- Solvent Evaporation technique was suitable for the preparation of Tiagabine loaded PLGA and PEG-PLGA nanoparticles with high encapsulation efficiency. This formulation approach could be used to improve the therapeutic efficacy of poorly soluble drugs. The changes in nanoparticle size and release kinetics were affected by changes in polymer and stabilizer concentration. The controlled release of drug from the Tiagabine loaded nanoparticles suggested that the frequency of administration, dose and adverse effects of this molecule could be reduced. We can conclude that there is large scope for improving the use of Tiagabine Hydrochloride in Epilepsy treatments through nanoparticle as a drug delivery system. newline