Formulation and evaluation of nanosuspension of Lercanidipine HCl

Abstract

The main objective of the present study was to increase the aqueous solubility of poorly soluble Lercanidipine HCl and improve the bioavailability. Lercanidipine is mainly used as antihypertensive drug. The present work was focused on formulation of Lercanidipine HCl loaded nanoparticles using biodegradable polymer chitosan of low molecular weight by ionic gelation method using tripolyphosphate as cross linking agent, tween 80 as stabilizer. The nanoparticles were evaluated for various parameters like particle size, zeta potential, drug entrapment efficiency, surface morphology, in-vitro drug diffusion study and stability studies. FT-IR and DSC studies depicted that there was no interaction between drug and polymer. The drug entrapment efficiency was found to be in the range of 74.67 to 84.34%. The developed nanoparticles size was ranging from 106.23-360.17nm. The polydispersity index was found to be in the range of 0.015-0.451. Scanning electron microscopy studies revealed that particles were of irregular shape showing no agglomeration. The zeta potential was found to be in the range of +35.22 to +40.17mV. In-vitro drug diffusion study showed that the highest percentage cumulative drug release was found 84.41% for (F3) formulations in 12h. Kinetic modelling revealed that the in-vitro drug release follows first order kinetics and non-fickian drug release. Stability study revealed that there is no significant change in physicochemical properties, drug entrapment efficiency 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 and effective in-vitro release and in-vivo results.