Formulation and Optimization of Sustained Release Microparticles of Ketoprofen

Microparticles are one of the drug delivery systems used to sustain the release of drugs. The purpose of this work was to forumlate sustained-release microparticles of ketoprofen (KTP) for ocular delivery. The microparticles were prepared by the method of quasi emulsion-solvent diffusion using the design of experiments, the MINITAB 16 was used to analyze the results. EC:KTP mass ratio (%), PVA concentration (m/v %) and stirring speed (rpm) were selected as factors. Encapsulation efficiency rate (EE%) and in vitro release after 6h (REL6%) were selected as responses. The central composite design (CCD) was used for the formulation optimization. The results indicated that the optimal microparticles formulated has an EE = 78.89%, REL6% = 39.98% for a EC:KTP mass ratio = 80.59%, PVA concentration = 0.52% and stirring speed = 477.11 rpm. The optical microscope was used to determine the morphology of the optimized microparticles, they were of spherical shape. The in vitro dissolution at 35 °C in a medium with pH = 7.4 gave a sustained release in which 36.98% of ketoprofen was released after 6 h. According to the results obtained, the microparticles of ketoprofen can be used for the ocular sustained release.