Abstract

FORMULATION AND EVALUATION OF CHITOSAN NANOPARTICLES OF ROPINIROLE HCL TO TARGET BRAIN IN THE TREATMENT OF PARKINSON’S DISEASE

Anudeep Balla* and Divakar Goli

ABSTRACT

The aim of the current research is to develop chitosan nanoparticles of Ropinirole HCl to target the brain. Drug characterization was done by UV, Melting point analysis, DSC and FTIR. Drug excipient compatibility showed no possible interaction between drug and excipients. Ten formulations (CNP 1 to CNP 10) were prepared by varying the ratios of Chitosan (0.2%, 0.5%) and STPP (0.2%). The % encapsulation efficiency was found to be ranging from 14.35±0.29 to 69.14±0.23 %. The loading capacity was found to be ranging from 0.18±0.004 to 0.86±0.003 mg/ml and showed a linear relationship with encapsulation efficiency. The mean particle size was found to be ranging between 275.5 nm and 601.3 nm and result quality report was found to be good for all formulations. All formulations were found to be homogenous (less polydisperse) with polydispersity index values ranging from 0.147 to 0.274 (closer to zero). The zeta potential of all formulations was found to be positive with values ranging from 15.97 to 35.27 mV. In vitro diffusion studies were carried for all formulations and the drug release ranged from 29.70±1.24 to 80.56±1.97 after 24 h. From the kinetic studies, nanoparticles were found to be following Higuchi model indicating drug release mechanism was by diffusion. The n value from korsemeyer peppas plot was below 0.5 for all formulation indicating fickian diffusion. Results of in vivo BBB crossing study showed that when compared with pure drug, the formulated nanoparticles (CNP 2) carried the drug to brain effectively. Stability studies performed at room temperature (25±2° C) and refrigerator (3-5±2° C) showed no significant changes upon storage.

Keywords: Brain targeting, Chitosan, Ropinirole HCl, BBB.