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目的:通过优化处方和工艺制备缓释、长效的阿魏酸脂质体植入制剂。方法:采用HPLC测定阿魏酸含量,流动相乙腈-0.1%磷酸(22∶78),检测波长324 nm。运用醋酸钙主动载药技术制备阿魏酸脂质体,使用透析法考察阿魏酸脂质体的释放度。通过单因素试验考察磷脂材料、胆固醇含量、粒径及不同血液成分对阿魏酸脂质体释放度的影响,利用温敏凝胶技术进一步延长阿魏酸脂质体的缓释效果。结果:阿魏酸脂质体选择氢化大豆磷脂(HSPC)为脂质体膜材,HSPC与胆固醇的摩尔比4∶1,超声时间1 min,脂质体平均粒径397.7 nm,可实现12 h缓释效果,血液成分能够加速脂质体的释放但不同血液成分无显著性差异。采用温敏凝胶技术可延长阿魏酸脂质体的缓释效果,体外释药符合Higuchi方程且持续释放时间>48 h。结论:胎牛血清和大鼠血浆可替代人血清用于阿魏酸脂质体的释放度考察。通过控制脂质体的处方与工艺因素,并结合温敏凝胶技术可实现阿魏酸脂质体的缓释、长效。
OBJECTIVE: To prepare sustained-release and long-lasting ferulic acid liposomes by optimized formulation and technology. Methods: The content of ferulic acid was determined by HPLC. The mobile phase was acetonitrile-0.1% phosphoric acid (22:78). The detection wavelength was 324 nm. Ferulic acid liposomes were prepared by calcium acetate active drug loading technique and the release of ferulic acid liposomes was investigated by dialysis. The influence of phospholipid material, cholesterol content, particle size and different blood components on the release of ferulic acid liposomes was investigated by single factor test. The temperature-controlled gel technique was used to further prolong the sustained release of ferulic acid liposomes. Results: Ferulic acid liposomes were selected as liposome membranes, the molar ratio of HSPC to cholesterol was 4:1, ultrasonic time was 1 min, average diameter of liposomes was 397.7 nm, Slow release effect, blood components can speed up the release of liposomes but no significant difference between the different blood components. The use of temperature-sensitive gel technology can prolong the sustained release of ferulic acid liposomes, in vitro release consistent Higuchi equation and sustained release> 48 h. Conclusion: Fetal bovine serum and rat plasma can replace human serum for the release of ferulic acid liposomes. By controlling the prescription of liposomes and the process factors, combined with the thermo-sensitive gel technology, the sustained-release and long-term effects of ferulic acid liposomes can be achieved.