2007 年 127 巻 11 号 p. 1851-1862
A novel approach which had foreground of industrialization, surface liquid spraying, was studied in this paper to prepare biodegradable polylactic-co-glycolic acid (PLGA) microspheres for controlled release drug delivery system. To compare with the normal methods, the microspheres prepared by this approach were characterized by particle size distribution and photograph of microscope. The relationship between the particle size and the instrument parameters of novel method was set up for the first time. The central composite design (CCD) was applied to study the main effects and interactions of three instrument factors on preparation of microspheres. The particle size of microspheres was below 200 μm and the shape of microspheres was spherical in nature evidenced by microscope photographs. Vinpocetine was used as the model drug to prepare the vinpocetine PLGA microspheres (VIN-PLGA-MS), and then drug loading, entrapment efficiency, scanning electron microscopy (SEM), Differential Scanning Calorimetry (DSC) and in vitro drug release behavior were examined. The results indicated that the drug loading and entrapment efficiency were increased using the novel method. The drug released slowly more than 30 days. The release behavior was fit for four kinds of kinetic model. The result indicated that release behavior was fitted by Zero-order kinetic model before release 72 hours, and was fitted with First-order kinetic model after release 72 hours. The novel method developed in our paper can give a promising way for industrialization, and the foreground was also proved by the scale-up batch experiment.
