白藜芦醇/siRNA胶束复合物的载药和释药性能研究

Study on drug loading and drug release properties of Resveratrol /siRNA micellar polyplexes

目的研究pH和还原性双响应白藜芦醇/siRNA胶束复合物(MCpH/Redox@Res-siRNA)的载药和释药性能。方法采用紫外分光光度法和荧光分光光度法分别建立白藜芦醇(Resveratrol,Res)和FAM-siRNA体外分析方法,超速离心法和超滤离心法测定MCpH/Redox@Res-siRNA中药物的包封率(Encapsulation Efficiency,EE%)和载药量(Drug Loading,DL%),透析法测定MCpH/Redox@RessiRNA中药物的释放性能。结果Res和FAM-siRNA的体外分析方法均符合方法学要求;MCpH/Redox@Res-siRNA中Res的EE%为(92.2±1.74)%、DL%为(9.72±1.63)%,FAM-siRNA的EE%为(94.5±1.42)%;MCpH/Redox@Res-siRNA中Res释放具有pH敏感性,siRNA的释放呈现pH和还原环境依赖性,在pH 5.5和还原性环境中,Res和FAM-siRNA释放较为迅速和完全。结论MCpH/Redox@Res-siRNA具有较好的Res和siRNA载药性能和释放性能。

Objective To study the drug loading and drug release properties of pH and reducing double-responsive Resveratrol/siRNA micellar polyplexes(MCpH/Redox@Res-siRNA).Methods UV spectrophotometry and fluorescence spectrophotometry were established for Resveratrol(Res)and FAM-siRNA in vitro respectively.Encapsulation Efficiency(EE%)and Drug Loading(DL%)of Res and FAM-siRNA in MCpH/Redox@Res-siRNA were determined by ultrafiltration centrifugal method and ultrafiltration centrifugal method.The drug release properties in MCpH/Redox@Res-siRNA was detected by dialysis.Results The EE%of Res and DL were(92.2±1.74)%,(9.72±1.63)%in MCpH/Redox@Res-siRNA.The EE%of FAM-siRNA were(94.5±1.42)%.The release of Res in MCpH/Redox@Res-siRNA was pH-responsive,and the release of siRNA is pH and reducing environment dependent.In pH5.5 and reducing environment,the release of Res and FAM-siRNA is rapid and complete.Conclusion MCpH/Redox@Res-siRNA have good Res and siRNA delivery and release properties.