大黄素soluplus聚合物胶束的制备及质量评价

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。

Preparation and Quality Evaluation of Emodin-loaded Soluplus Polymeric Micelles

Objective: To prepare emodin-loaded soluplus polymeric micelles (Emo-PMs) and evaluate their quality. Method: Emo-PMs were prepared by film dispersion method using an amphiphilic copolymer soluplus.Emo-PMs were characterized by particle size analyzer, transmission electron microscopy (TEM), X-ray diffraction (XRD);release curve was determined by dynamic membrane dialysis;HPLC was employed to determine entrapment efficiency and drug loading with mobile phase of methanol-0.1% phosphoric acid(75:25) and detection wavelength ar 437 nm. Result: Emo-PMs showed spherical with a mean particle size of (65±3.8)nm, polydispersity index of 0.099±0.022, Zeta potential of-(12.7±0.19) mV, average encapsulation efficiency of (88.25±3.51)% and average drug loading of (4.51±0.72)%.Emodin entrapped in polymer micelles with amorphous or molecular form;release methanism of Emo-PMs fitted Higuchi equation. Conclusion: These prepared Emo-PMs had exhibited in vitro sustained release, their particle size, encapsulation efficiency and drug loading were controllable.