Abstract

FABRICATION OF PLGA NANOPARTICLES OF ROPINIROLE HCL BY EMULSION SOLVENT EVAPORATION TECHNIQUE TO TARGET BRAIN

Anudeep Balla*, Ashvini H. M. and Divakar Goli

Abstract

The aim of the current research is to develop PLGA 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. A general full factorial design was constructed using Minitab 17 statistical software. Nine formulations were prepared with two factors PLGA and PVA with 3 levels each. The % encapsulation efficiency was found to be ranging from 57.31±0.82 to 85.13±0.29%. The loading capacity was found to be ranging from 0.96±0.014 to 1.42±0.005 mg/ml and showed a linear relationship with encapsulation efficiency. The mean particle size was found to be ranging between 224.3 nm to 581.9 nm and result quality report was found to be good for all formulations except F5 and F9. All formulations except F9 & F5 (PDI value of 1 and 0.643 respectively) were found to be homogenous (less polydisperse) with polydispersity index values ranging from 0.052 to 0.382 (closer to zero). The zeta potential of all formulations was found to be near neutral with values ranging from -3.64 to -0.14 mV. In vitro diffusion studies were carried for all formulations and the drug release ranged from 35.17±1.63 to 79.46±1.08 after 48 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 (F2) carried the drug to brain effectively. Stability studies performed at refrigerator conditions (3-5±2°C) showed no significant changes upon storage.

Keywords: Brain targeting, PLGA, PVA, Emulsion solvent evaporation, Ropinirole HCl, BBB.