白屈菜红碱脂质体-温敏凝胶的制备及体外释放研究

Prescription and in vitro release of Chelerythrine Liposome-temperature sensitive gel

目的:优选白屈菜红碱(CHE)脂质体-温敏凝胶的制备工艺,考察其性质及体外释放特征。方法:采用"冷溶法"以泊洛沙姆407(P407)和泊洛沙姆188(P188)为凝胶基质,以胶凝温度为考察指标优化CHE脂质体-温敏凝胶制备工艺;HPLC分析方法测定CHE含量,透析法考察体外释放特征。结果:优化处方用量为磷脂浓度8mg·m L^(-1)、磷脂胆固醇比8∶1、药脂比1∶7、有机相水相比1∶3、P-407与P-188比20%:6%;所制得CHE脂质体-温敏凝胶粒径、包封率、载药量、胶凝温度分别为113.8nm,76.27%,8.84%,35.5℃;体外释放结果显示,CHE脂质体温敏凝胶24h内累计释放率为54.73%,48h内累计释放率为64.01%。结论:制得的CHE脂质体-温敏凝胶具有温敏特性及良好的缓释效果。

OBJECTIVE:The preparation process of chelerythrine(CHE)liposome-temperature sensitive gel is preferred, and its properties and in vitro release characteristics are investigated. METHODS: Using"cold-dissolving method"with poloxamer 407(P407) and poloxamer 188(P188) as gel matrix, the gelatinization temperature was used as an index to optimize the preparation process of chelerythrine liposome-temperature sensitive gel. The content of chelerythrine was determined by HPLC analysis, and the in vitro release characteristics were investigated by dialysis method. RESULTS: Optimized prescription dosage is phospholipid concentration 8 mg·mL^-1, phospholipid cholesterol ratio 8:1, drug-to-fat ratio 1∶7, organic phase water ratio 1∶3, P-407 and P-188 ratio 20%: 6%;The particle size, encapsulation efficiency, drug loading, and gelation temperature of the chelerythrine liposome-temperature sensitive gel prepared were 113.8 nm, 76.27%, 8.54%, and 35.5°C, respectively;The in vitro release results showed that the cumulative release rate of chelerythrine liposome thermosensitive gel within 24 h was54.73%, and the cumulative release rate within 48 h was 64.01%. Conclusion: The prepared chelerythrine liposome-thermosensitive gel has temperature-sensitive properties and good sustained release effect.