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目的:以姜黄素为模型药物,制备Pluronic F127聚合物的载药胶束并阐明Pluronic F127在水中的胶束化过程。方法:采用HPLC测定姜黄素含量,流动相0.1%甲酸水溶液-甲醇(30∶70),检测波长420 nm。采用薄膜水化法制备姜黄素Pluronic F127胶束,通过正交试验考察姜黄素-Pluronic F127质量比、水相用量、水相pH和水化时间对载药共聚物胶束包封率及载药量的影响。利用动态光散射法测定胶束粒径,动态透析法考察载药胶束的体外释放行为,并通过1H-NMR分析Pluronic F127在水中的胶束化行为。结果:优选的处方工艺为姜黄素-Pluronic F127(1∶15),水相用量10 mL,水相pH 5.0,水化时间1.0 h。姜黄素Pluronic F127胶束的平均粒径约30 nm,平均包封率64.5%,平均载药量4.1%,体外释放符合Higuchi方程。在水中随着Pluronic F127质量浓度的增高,质子的NMR化学位移向高场移动且信号变宽。结论:Pluronic F127在水中已形成了可载药的疏水性胶束内核,Pluronic F127具有优良的载药及缓释能力。
OBJECTIVE: To prepare drug-loaded micelles of Pluronic F127 with curcumin as a model drug and elucidate the micellarization of Pluronic F127 in water. Methods: The content of curcumin was determined by HPLC. The mobile phase consisted of 0.1% formic acid in methanol (30:70) and the detection wavelength was at 420 nm. The curcumin-Pluronic F127 micelles were prepared by the membrane hydration method. The orthogonal test was used to investigate the effects of curcumin-Pluronic F127 mass ratio, aqueous phase, pH and hydration time on the entrapment efficiency and drug loading The impact of volume. The size of micelles was determined by dynamic light scattering method. The in vitro release behavior of drug-loaded micelles was investigated by dynamic dialysis. The micellarization of Pluronic F127 in water was analyzed by 1H-NMR. Results: The optimal prescription was curcumin-Pluronic F127 (1:15), the amount of aqueous phase was 10 mL, the aqueous phase was pH 5.0 and the hydration time was 1.0 h. Curcumin Pluronic F127 micelles average particle size of about 30 nm, the average entrapment efficiency of 64.5%, the average drug loading 4.1%, in vitro release in line with Higuchi equation. As the mass concentration of Pluronic F127 increases in water, the NMR chemical shifts of the protons move to higher fields and the signal broadens. Conclusion: Pluronic F127 has formed a drug-loaded hydrophobic micellar core in water. Pluronic F127 has excellent drug loading and sustained release ability.