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Abstract

Formulation & Evaluation of PLGA Nanoparticles of Ropinirole HCl for Targeting Brain

Author(s): ANUDEEP BALLA1*, DIVAKAR GOLI
Department of pharmaceutics, Acharya & BM Reddy College of Pharmacy, Bengaluru, India

Correspondence Address:
Department of pharmaceutics, Acharya & BM Reddy College of Pharmacy, Bengaluru, India, E-mail: [email protected]

The current research was aimed at formulating brain targeting polymeric nanoparticles of a hydrophilic anti-parkinson agent (Ropinirole HCl) to improve the drug passage to brain. Two different approaches were used for the study. One was Chitosan nanoparticles prepared by ionic gelation method using tripolyphosphate as cross-linking agent and the other one was poly (lactic-co-glycolic acid)50:50 monomer ratio poly D,L-lactic-co-glycolic acid nanoparticles prepared by a modified two step nanoprecipitation method using polyvinyl alcohol as stabilizer. Polysorbate-80 was used to coat the nanoparticles to further improve its passage through brain. Minitab 17 statistical software was employed to create general full factorial design. Drug-excipient compatibility study by Fourier transform infrared spectroscopy and differential scanning calorimetry revealed no possible interactions. Kinetic modelling of in vitro release showed that poly D,L-lactic-co-glycolic acid nanoparticles were more linear towards KorsemeyerPeppasmodel indicating drug release from the nanoparticles was by a combination of bulk degradation followed by diffusion (Fickian diffusion). The scanning electron microscopy studies showed that poly D,L-lactic-co-glycolic acid nanoparticles were found to be spherical with either smooth or rough at surface. Stability studies performed at refrigerator conditions (3-5±2º) showed no significant changes upon storage. Results of in vivo blood brain barrier crossing study showed that when compared with pure drug, the formulated nanoparticles carried the drug to brain effectively. Owing to the lower particle size and pharmacy and drug information, poly D,L-lactic-co-glycolic acid nanoparticles were able to pass through blood brain barrier effectively than chitosan nanoparticles. Also, the ability of poly D,L-lactic-co-glycolic acid to release drug in a sustained manner for weeks makes it a promising drug delivery system.

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