辅酶Q10纳米乳剂的研制及经皮性能考察

Preparation and transdermal properties study of coenzyme Q10 nanoemulsion

目的制备经皮透过量低,滞留量高的可用于皮肤护理的辅酶Q10(coenzyme Q10,Co-Q10)水包油型纳米乳。方法以滞留比为指标,对以聚乙二醇1000维生素E琥珀酸酯(tocopheryl polyethylene glycol 1000 vitamin E succinate, TPGS)为主要乳化剂的纳米乳进行处方优化,筛选出最佳处方。以日本大耳白兔离体皮肤作为透皮模型,采用立式扩散池,进行离体经皮渗透试验并测定Co-Q10的含量。结果优化后的最终纳米乳处方组成为:中链甘油三酯(medium chain triglycerides, MCT)1 g,甘油3.34 g, TPGS 1.66 g,水4 g, Co-Q10 50 mg。纳米乳粒径为32.2 nm,多分散指数(polydispersity index, PDI)为0.177。折光率为1.336 5,黏度为59.8 mPa·s。测定Co-Q10的8 h的滞留量为37.66μg·cm-2,滞留比为1.93。结论该制剂药物有一定的通过率,滞留比高,适合于局部给药。

Objective To optimize the preparation of coenzyme Q10(Co-Q10) transdermal nanoemulsion with the low skin permeability and the high retention capacity.Methods Using the retention ratio as an indicator, the formulation of nanoemulsion with tocopheryl polyethylene glycol 1000 vitamin E succinate(TPGS) as the main emulsifier was optimized, and the best prescription was screened out.Percutaneous penetration tests were performed with vertical diffusion cells using rabbit skin in vitro to determine the content of Co-Q10.Results The optimized composition of the nanoemulsion was MCT:1 g, glycerol: 3.34 g, TPGS:1.66 g, water: 4 g, and Co-Q10:50 mg.The particle size of nano-emulsion was 32.2 nm with the PDI of 0.177,refractive index of 1.336 5,and the viscosity of 59.8 mPa·s.The 8-hour rabbit skin retention of Co-Q10 was 37.66 μg·cm-2,and the retention ratio was 1.93.Conclusion This optimized prescription has a high retention ratio and is suitable for topical administration.