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目的:制备大黄素的soluplus聚合物胶束并对其进行质量评价。方法:采用薄膜分散法制备大黄素聚合物胶束(Emo-PMs)。利用粒径测定仪、透射电镜、X-射线衍射对其进行表征;采用HPLC测定Emo-PMs的包封率和载药量,流动相甲醇-0.1%磷酸(75∶25),检测波长437 nm;采用动态膜透析法考察载药胶束的体外释药特性。结果:Emo-PMs呈球形或类球形,平均粒径(65±3.8)nm,多分散系数0.099±0.022,Zeta电位-(12.7±0.19)mV,平均包封率(88.25±3.51)%,平均载药量(4.51±0.72)%;大黄素以无定形状态或分子状态包载在聚合物胶束中;Emo-PMs具有缓释作用,释放机制符合Higuchi方程。结论:制备的Emo-PMs粒径、包封率、载药量可控,具有缓释作用。
Objective: To prepare emodin soluplus polymer micelles and evaluate their quality. Methods: Emodin polymer micelles (Emo-PMs) were prepared by membrane dispersion method. The entrapment efficiency and drug loading of Emo-PMs were determined by using particle size analyzer, transmission electron microscopy and X-ray diffraction. The mobile phase consisted of methanol-0.1% phosphoric acid (75:25), the detection wavelength was 437 nm The dynamic release characteristics of drug-loaded micelles in vitro were investigated by dynamic membrane dialysis. RESULTS: Emo-PMs were spherical or spheroidal with an average size of 65 ± 3.8 nm, polydispersity 0.099 ± 0.022 and Zeta potential 12.7 ± 0.19 mV, with an average entrapment efficiency of 88.25 ± 3.51% (4.51 ± 0.72)%. Emodin was entrapped in polymer micelles in an amorphous or molecular state. Emo-PMs exhibited sustained release and the release mechanism was in accordance with the Higuchi equation. Conclusion: The prepared Emo-PMs can be controlled in particle size, entrapment efficiency and drug loading, with sustained release.