摘要
采用预聚—扩链—中和法合成松香基聚氨酯(RPU),以其为载体,以5-氟尿嘧啶(5-Fu)为模型药物,通过悬浮聚合法制备了负载5-Fu的松香基聚氨酯微球(5-Fu/RPUMs)。采用单因素实验优化了药物负载条件,通过红外光谱、X射线光电子能谱、扫描电子显微镜、能谱分析等对载药微球进行表征,研究了载药微球的体外释放性能及药物释放动力学模型。结果表明:成功制备了5-Fu/RPUMs微球,平均粒径为35.0μm,表面光滑圆整且有孔。药物最佳负载条件为:ρ_(5-Fu)=120 mg/mL,致孔剂种类为正丁醇/甲苯,此条件下RPU对5-Fu的包封率达63.35%,载药量达7.60%。5-Fu/RPUMs在不同pH下表现出不同的缓释性能,具有pH敏感性;在pH=6.8的PBS缓冲溶液中,264 h后的累积释放率为65.80%,具有长效的缓释作用。
Rosin-based polyurethane microspheres(5-Fu/RPUMs)are prepared by suspension polymerization using 5-fluorouracil(5-Fu)as the model drug rosin-based polyurethane(RPU)synthesized by prepolymerization,and extension and neutralization method as the carrier single factor experiment is used to optimize drug-loaded conditions.Infrared spectrometer X-ray photoelectron spectroscopy,scanning electron microscopy and energy dispersive spectrometer are used to characterize drug-loaded microspheres.The in-vitro release performance and drug release kinetics model of drug-loaded microspheres are studied.The results show that 5-Fu/RPUMs are successfully prepared with an average particle size of 35.0μm and a smooth,rounded surface with holes.The optimal loading conditions are ρ_(5-Fu)=120 mg/mL and n-butanol/toluene as pore-forming agent.Under these conditions,the encapsulation rate of RPU to 5-Fu reaches 63.35%and the drug loading is 7.60%.5-Fu/RPUMs is pH sensitive showing different sustainable release at different pH.In PBS buffer solution with pH=6.8,the cumulative release rate after 264 h is 65.80%,showing a long-acting sustainable release effect.
作者
严成飞
张发爱
邵金涛
余彩莉
YAN Chengfei;ZHANG Faai;SHAO Jintao;YU Caili(College of Chemical and Biology Engineering,Guilin University of Technology,Guilin 541006,China;College of Materials Science and Engineering,Guilin University of Technology,Guilin 541006,China)
出处
《桂林理工大学学报》
CAS
北大核心
2024年第1期155-161,共7页
Journal of Guilin University of Technology
基金
国家自然科学基金项目(51863007)。
关键词
松香
聚氨酯微球
载药
释放
rosin
polyurethane microspheres
drug-loaded
release
