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研制CI-921混合胶束(CI-Micelles),建立CI-Micelles包封率的测定方法,并对胶束进行处方优化和体外表征。采用薄膜分散法制备CI-Micelles,通过透析法分离CI-Micelles的游离药物和载药胶束,测定药物含量,得到包封率和载药量的测定值,利用方程拟合法推算出CI-Micelles包封率和载药量的真实值。考察聚合物的总量、两种聚合物用量的比例和水合介质的种类对胶束粒径分布、包封率和载药量的影响;考察载药胶束4℃下6 d内的放置稳定性。结果表明,以总聚合物浓度为72 mg/m L,Pluronic F127与Solutol HS15质量之比为1∶2,5%葡萄糖溶液为水合介质时制备的CI-Micelles具有最佳的包封率(>90%)和粒径分布(17~25 nm,分布系数<0.210),在4℃下放置6 d,包封率及粒径均无显著变化。本实验所建立的新型包封率的测定方法——透析拟合法可以用来考察难以达到漏槽条件的弱碱性药物小粒径胶束的包封率。利用混合配比的聚合物材料Pluronic F127和Solutol HS15制备的CI-Micelles粒径分布均匀,包封率和载药量高,稳定性较好。
CI-921 mixed micelles (CI-Micelles) were developed to determine the entrapment efficiency of CI-Micelles. The micelles were optimized for formulation and characterized in vitro. CI-Micelles was prepared by thin-film dispersion method. The free drug and drug-loaded micelles of CI-Micelles were separated by dialysis method. The drug content was determined and the entrapment efficiency and drug loading were measured. The CI-Micelles Encapsulation efficiency and drug loading of the real value. The effects of the total amount of the polymer, the ratio of the two polymers and the type of the hydration medium on the particle size distribution, entrapment efficiency and drug loading of the micelles were investigated. The stability of the drug-loaded micelles was observed within 6 days at 4 ℃ Sex. The results showed that CI-Micelles prepared with a total polymer concentration of 72 mg / mL, a mass ratio of Pluronic F127 to Solutol HS15 of 1: 2, and a 5% glucose solution used as a hydration medium exhibited the best entrapment efficiency (> 90%) and particle size distribution (17 ~ 25 nm, distribution coefficient <0.210). After being stored at 4 ℃ for 6 days, the encapsulation efficiency and particle size did not change significantly. The new method of determination of entrapment efficiency established by this experiment - dialysis fitting method can be used to investigate the entrapment efficiency of small-size drug-eluting micelles which is difficult to reach the condition of draining groove. The CI-Micelles prepared by using Pluronic F127 and Solutol HS15 with uniform mixing ratio had uniform particle size distribution, high entrapment efficiency and drug loading, and good stability.