星点设计-效应面法优化莫匹罗星微乳透皮给药系统

Optimization of the transdermal microemulsion drug delivery system of mupirocin by central composite design-response surface methodology

目的筛选及优化莫匹罗星微乳经皮给药系统。方法采用HPLC方法测定莫匹罗星在各辅料中的饱和溶解度和绘制伪三元相图,确定微乳处方所用辅料及K_m值。以粒径、稳定性及皮肤滞留量为考察指标,通过星点设计-效应面法优化微乳制剂处方。结果经过处方筛选及优化,确定莫匹罗星微乳最优处方为:20.3%MAISINE 35-1、13.23%吐温80、13.23%LABRASOL、26.46%TRANSCUTOLP和26.78%水。微乳粒径均匀,稳定性较好,皮肤滞留量为(45.07±2.03)mg·g^(-1),符合透皮微乳要求。结论本实验制得了符合要求的莫匹罗星微乳,为进一步研究奠定了良好的基础。

AIM To screen and optimize the formulation of mupirocin microemulsion transdermal delivery system. METHODS Mupimcin use as indexes, its saturated solubility in various materials was determined by HPLC and initially identified several materials in which mupirocin＇s solubility was greater. Then pseudo-ternary phase diagrams were drawn and primary compositions and Km values of microemulsion formulation according to the area of microemulsion in phase di- agrams were obtained. Finally, the formulation was optimized by central composite design and its quality indexes including particle size, stability and the amount of mupimcin retention in the skin were determined. RESULTS After screening and optimization, the optimal mupirocin microemulsion formulation was： 20.3 % MAISINE 35-1,13.23 % Tween 80, 13.23% LABRASOL, 26.46% TRANSCUTOL P and 26.78% water. The microemulsion equipped with uniform particle size, good stability and retention amount [ （45.07± 2.03） mg·g^-1] in skin was accorded with the requirement of transdermal microemuslion. CONCLUSION The optimal mupirocin microemulsion has the characteristics of uniform particle size, good stability and retention amount, which provides a good foundation for further study.