姜黄素mPEG114-PCL36纳米胶束的制备及体外释药考察

目的:制备载姜黄素mPEG114-PCL36纳米胶束并考察其体外释药情况.方法:利用开环聚合法合成聚乙二醇单甲醚-聚己内酯(mPEG114-PCL36)嵌段共聚物,通过FT-IR和1H-NMR确证其结构,芘荧光探针法测定其临界胶束浓度.采用透析法制备姜黄素聚合物胶束,通过正交试验考察共聚物质量浓度、姜黄素质量浓度、水相与有机相的体积比对包封率、载药率和胶束粒径的影响.利用HPLC测定载药率、包封率,激光散射法测定粒径,动态透析法考察体外释药特性.结果:制备的纳米胶束平均粒径(48.5±1.7) nm,粒径多分散系数(0.20±0.07),包封率(49.12±1.26)％,载药率(4.46±0.12)％,72 h体外累计释放率41.9％,无明显突释现象.结论:透析法制备的姜黄素mPEG-PCL纳米胶束粒径小且分布均匀,具有良好的缓释性能.

Preparation and in vitro Release Investigation of Curcumin-Loaded mPEG114-PCL36 Naonmicelles

Objective: To prepare curcumin-loaded mPEG₁₁₄-PCL₃₆ nanomicelles and investigate its in vitro release. Method: mPEG₁₁₄-PCL₃₆ block copolymer was synthesized by ring-opening polymerization method and its structures was identified by FT-IR and ¹H-NMR,the critical micelle concentration was detected by fluorescence techniques with pyrene as a probe.Polymer micelles containing curcumin were prepared by dialysis,effects of the concentration of copolymer and curcumin,volume ratio of aqueous phase to organic phase on particle size of micelles,entrapment efficiency and drug loading was evaluated by orthogonal design.Eencapsulation efficiency and drug loading were determined by HPLC,particle size was examined by laser light scattering,dynamic dialysis method was used to investigate in vitro release characteristic of nanomicelles. Result: Average particle size of these prepared nanomicelles was (48.5±1.7) nm with polydispersity index of (0.20±0.07),drug loading of (49.12±1.26)% as well as encapsulation efficiency of (4.46±0.12)%.In vitro cumulative release of curcumin nanomicelles in 72 h was 41.9% and without significant burst release at initial stage. Conclusion: These prepared curcumin-loaded nanomicelles showed a good sustained-release property with small and evenly distributed particle size.