School of Pharmacy, Shanghai Jiao Tong University, Shanghai, People’s Republicof China.
Int J Nanomedicine. 2011;6:1603-10. doi: 10.2147/IJN.S22667. Epub 2011 Aug 4.
The aim of this study was to develop new systems for transdermal delivery of paeonol, in particular microemulsion gel and cubic gel formulations.
Various microemulsion vehicles were prepared using isopropyl myristate as an oil phase, polyoxyethylated castor oil (Cremophor(®) EL) as a surfactant, and polyethylene glycol 400 as a cosurfactant. In the optimum microemulsion gel formulation, carbomer 940 was selected as the gel matrix, and consisted of 1% paeonol, 4% isopropyl myristate, 28% Cremophor EL/polyethylene glycol 400 (1:1), and 67% water. The cubic gel was prepared containing 3% paeonol, 30% water, and 67% glyceryl monooleate.
A skin permeability test using excised rat skins indicated that both the cubic gel and microemulsion gel formulations had higher permeability than did the paeonol solution. An in vivo pharmacokinetic study done in rats showed that the relative bioavailability of the cubic gel and microemulsion gel was enhanced by about 1.51-fold and 1.28-fold, respectively, compared with orally administered paeonol suspension.
Both the cubic gel and microemulsion gel formulations are promising delivery systems to enhance the skin permeability of paeonol, in particular the cubic gel.
本研究旨在开发丹皮酚的透皮给药新系统,特别是微乳凝胶和立方凝胶制剂。
采用肉豆蔻酸异丙酯作为油相、聚氧乙烯蓖麻油(Cremophor(R)EL)作为表面活性剂、聚乙二醇 400 作为助表面活性剂,制备了各种微乳载体。在最佳微乳凝胶配方中,选择卡波姆 940 作为凝胶基质,由 1%丹皮酚、4%肉豆蔻酸异丙酯、28%Cremophor EL/聚乙二醇 400(1:1)和 67%水组成。立方凝胶含有 3%丹皮酚、30%水和 67%单油酸甘油酯。
采用离体大鼠皮肤进行的皮肤渗透试验表明,立方凝胶和微乳凝胶制剂的渗透性均高于丹皮酚溶液。在大鼠体内药代动力学研究中,与口服丹皮酚混悬液相比,立方凝胶和微乳凝胶的相对生物利用度分别提高了约 1.51 倍和 1.28 倍。
立方凝胶和微乳凝胶制剂均是增强丹皮酚皮肤渗透性的有前途的给药系统,特别是立方凝胶。