Abstract

DESIGN, DEVELOPMENT AND EVALUATION OF NANOPARTICLES OF POORLY SOLUBLE VALSARTAN

Prajapati Maheshkumar D, GS Shantha Kumar*, Divakar Goli, Roopa Karki

ABSTRACT

The main objective of the present study was to decrease the particle size, reduce the dose frequency and increase the aqueous solubility of poorly soluble valsartan. In the present work an attempt was made to formulate valsartan loaded nanoparticles by ionic gelation followed by sonication method using different concentrations of biodegradable polymer chitosan of low molecular weight(1:1, 1:1.5 & 1:2) and tween 80(0.25%, 0.50% & 0.75%) as stabilizer. The nanoparticles were characterized for compatibility study, particle size, zeta potential, drug entrapment efficiency, surface morphology, in-vitro diffusion study, in-vivo antihypertensive studies and stability studies. FT-IR and DSC study showed that there was no interaction between drug and polymer. The particle size and polydispersity index of nanoparticles were found in the range of 91.68-226.67nm and 0.004-0.210 respectively. The zeta potential was found to be in the range of +33.28-+38.55mV and showed nanoparticles are stable. Highest drug entrapment efficiency was found to be 78.63% (F2). SEM studies showed that particles were of irregular shape with rough surface and no agglomeration. The in vitro drug diffusion study revealed that highest % CDR of 87.68% (F2) in 12h. Kinetic modelling revealed that the in-vitro drug release followed zero order kinetics and non-fickian diffusion drug release. From the in vivo studies it was predicted that there was a significant reduction in hypertension. Stability studies showed no significant differences in drug entrapment and in-vitro drug release. Thus, the prepared nanoparticles proved to be a potential candidate as by enhancing the aqueous solubility by reducing the particle size, effective in vitro drug release and significant reduction in hypertension.

Keywords: Nanoparticles, Valsartan, Chitosan, Ionic gelation, In vitro, Hypertension.