Institute of Chemical and Engineering Sciences, A*STAR (Agency for Science, Technology and Research), 1 Pesek Road, Jurong Island, Singapore, 627833, Singapore.
Institute of Chemical and Engineering Sciences, A*STAR (Agency for Science, Technology and Research), 1 Pesek Road, Jurong Island, Singapore, 627833, Singapore.
Colloids Surf B Biointerfaces. 2020 May;189:110823. doi: 10.1016/j.colsurfb.2020.110823. Epub 2020 Jan 23.
The aim of this work was to develop microemulsions and microemulsion gels which can be used as vehicles for the topical delivery of ivermectin. Tea tree oil and ethyl butanoate were found to be suitable for ivermectin-loaded microemulsion formulations due to the higher solubility of ivermectin in these two oils than other tested oils. The pseudo-ternary phase diagrams were constructed based on these selected oils and combination of different surfactant/co-surfactant at different ratios. Ivermectin-loaded stable microemulsions and microemulsion gels were successfully formulated based on the selected compositions from the phase diagrams. Ivermectin-loaded microemulsions showed spherical nano-droplets dispersed in the continuous phase (via cryogenic field emission scanning electron microscope image) and the particle size was less than 100 nm (via dynamic light scattering measurement). Ethyl butanoate based microemulsion appeared to be the best microemulsion formulation considering the stability and permeation profiles while tea tree oil based microemulsion showed the best stability profile. Overall, microemulsion gel formulations exhibited better stability profiles than their microemulsion counterparts. All microemulsion gel formulations demonstrated significantly faster in vitro membrane permeation (release) rate of ivermectin than Soolantra cream (reference marketed product by Galderma, USA).The developed microemulsion and microemulsion gel formulations appear to be promising vehicles for topical delivery of ivermectin.
本工作旨在开发可用于伊维菌素经皮传递的微乳液和微乳液凝胶。由于茶树油和丁酸乙酯中伊维菌素的溶解度高于其他测试油，因此发现它们适合用于载有伊维菌素的微乳液配方。基于这些选定的油和不同表面活性剂/共表面活性剂的不同比例，构建了伪三元相图。根据相图中选择的组成，成功地配制了载有伊维菌素的稳定微乳液和微乳液凝胶。载有伊维菌素的微乳液显示出分散在连续相中的球形纳米液滴（通过低温场发射扫描电子显微镜图像），粒径小于 100nm（通过动态光散射测量）。考虑到稳定性和渗透特性，丁酸乙酯基微乳液似乎是最佳的微乳液配方，而茶树油基微乳液则表现出最佳的稳定性。总的来说，微乳液凝胶配方的稳定性比其微乳液对应物要好。所有微乳液凝胶配方均表现出比 Soolantra 霜（美国 Galderma 的市售参考产品）更快的体外膜渗透（释放）伊维菌素速度。所开发的微乳液和微乳液凝胶配方似乎是伊维菌素经皮传递的有前途的载体。
