Acta Pharm. 64 (2014) 403-418

full paper

Original research paper

Influence of different formulations and process parameters during the preparation of drug-loaded PLGA microspheres evaluated by multivariate data analysis

JAKUB VYSLOUŽIL, PETR DOLEŽEL, MARTINA KEJDUŠOVÁ, ELIŠKA MAŠKOVÁ, JOSEF MAŠEK, ROBERT LUKÁČ, VRATISLAV KOŠŤÁL, DAVID VETCHÝ and KATEŘINA DVOŘÁČKOVÁ

dvorackovak@vfu.cz

¹ Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, 612 42 Brno, Czech Republic

² Department of Toxicology, Pharmacology and Immunotherapy, Veterinary Research Institute, 621 00 Brno, Czech Republic

³ Tescan, 62300 Brno-Kohoutovice, Czech Republic

Accepted June 16, 2014

The main objective of this study was to evaluate the influence of the formulation and process parameters on PLGA microparticles containing a practically insoluble model drug (ibuprofen) prepared by the o/w solvent evaporation method. Multivariate data analysis was used. The effects of altered stirring speed of a mechanical stirrer (600, 1000 rpm), emulsifier concentrations (PVA concentration 0.1 %, 1 %) and solvent selection (dichlormethane, ethyl acetate) on microparticles characteristics (encapsulation efficiency, drug loading, burst effect) were observed. It was found that with increased stirring speed, the PVA concentration or the use of ethyl acetate had a significantly negative effect on encapsulation efficiency. In addition, ethyl acetate had an adverse effect on the burst effect, while the increased stirring speed had the opposite effect. Drug load was not affected by any individual variable, but rather by the interactions of evaluated variables.

Keywords: solvent evaporation, encapsulation, PLGA, controlled release, burst effect