西罗莫司纳米结构脂质载体分散液的制备及其体外释放度考察

目的优化西罗莫司纳米结构脂质载体(sirolimus nanostructured lipid carriers,SRL-NLC)分散液的处方,并考察其体外释放度。方法采用星点设计-效应面法(central composite design-response surface methodology,CCD-RSM)优化SRL-NLC分散液的处方,并以粒径、分布系数、载药量和包封率作为评价指标,采用正相透析袋法考察SRL-NLC分散液在0.4%SDS(十二烷基硫酸钠)溶液中的释放度。结果经优化的SRL-NLC分散液平均粒径82.54 nm、分布系数0.207,Zeta电位-18.0mv、载药量1.829%和包封率91.3%,SRL-NLC分散液在0.4%SDS溶液中能持续释放120 h,累积释放量为60.1%。结论经优化的处方可行性和重现性均较好,SRL-NLC分散液在0.4%SDS溶液中累积释放度为60.1%。

Preparation and in vitro releasing of sirolimus-nanostructured lipid carriers dispension

Objective To optimize the preparation and study in vitro releasing of SRL-NLC dispersion. Methods Central composite design-response surface methodology was used to optimize dispersion formulation,then in vitro releasing in 0.4% SDS(sodium lauryl sulfate) solution was explored by normal phase dialysis bag method. Results The optimal dispersion had PS(particle size):82.54nm,PI(polydisperity index):0.207, Zeta potential: -18.0 mv,DL (drug-loading): 1.829%, and EE(entrapment efficiency): 91.3%; SRL-NLC dispersion had a characterization of 60.1% accumulated releasing in 0.4%SDS solution. Conclusion The optimal formulation had good feasibility and reproducibility, in vitro releasing curve showed SRL-NLC dispersion had a characterization of 60.1% accumulated releasing in 0.4% SDS solution.