关键词: 制备, 优化设计, 载体, 壳聚糖, 明胶, 5-氟尿嘧啶, 体外释药

Abstract: Chitosan and Gelatin are good biocompatible polymers and are suitble for drug carriers. Preparation of 5-fluorouracil loaded chitosan/gelatin particles and in vitro release were performed using emulsion crosslinking method with paraffin oil as external phase and chitosan/gelatin as internal phase, and the optimal formulations were verified by orthogonal design. The drug loading, encapsulation efficiency, the microscopic morphology and release behavior of drug loaded particles in vitro were examined. The optimal preparation conditions were:the ratio of water to oil 1:7, the ratio of chitosan/gelatin concentration 1:3, emulsifying time 5min, emulsifying temperature 60℃, glutaraldehyde dosage 5.5mmol/L, reaction time 1h, and emulsifier dosage 100.7mmol/L. Under these conditions, the drug loading of particles was 34.96% and encapsulation efficiency was 38.36%. Infrared spectroscopy showed that chitosan/gelatin microparticles have loaded 5-Fu. Microparticles were spherical with smooth surface. 5-Fu can be encapsuoed in chitosan/gelatin by emulsion crosslinking method. This method was simple and reproducible and drug release performance in vitro showed that the microparticles had obviously sustained release effect.

Key words: preparation, optimal design, support, chitosan, gelatin, 5-fluorouracil, in vitro drug release