Department of Pharmaceutics, Faculty of Pharmacy, Al-Arab Medical University, Benghazi 5341, Libya.
Colloids Surf B Biointerfaces. 2010 Jan 1;75(1):356-62. doi: 10.1016/j.colsurfb.2009.09.010. Epub 2009 Sep 13.
Recently caffeine has been investigated for the treatment of various types of cancers upon oral administration. There is also some evidence that dermally applied caffeine can protect the skin from skin cancer caused by sun exposure. Therefore nanoemulsion formulation of caffeine for transdermal drug delivery was developed and evaluated in the present investigation. Different w/o nanoemulsion formulations of caffeine were prepared by oil phase titration method. Thermodynamically stable nanoemulsions were characterized for morphology, droplet size, viscosity and refractive index. The in vitro skin permeation studies were performed on Franz diffusion cell using rat skin as permeation membrane. The in vitro skin permeation profile of optimized formulation was compared with aqueous solution of caffeine. Significant increase in permeability parameters was observed in nanoemulsion formulations (P<0.05) as compared to aqueous solution of caffeine. The steady-state flux (J(ss)) and permeability coefficient (K(p)) for optimized nanoemulsion formulation (C12) were found to be 147.55+/-8.21 microg/cm(2)/h and 1.475 x 10(-2)+/-0.031 x 10(-2)cm/h, respectively. Enhancement ratio (E(r)) was found to be 17.37 in optimized formulation C12 compared with other formulations. Overall these results suggested that w/o nanoemulsions are good carriers for transdermal delivery of caffeine.
最近，人们研究了通过口服咖啡因来治疗各种类型的癌症。还有一些证据表明，局部应用咖啡因可以保护皮肤免受阳光照射引起的皮肤癌。因此，本研究开发并评价了咖啡因的纳米乳剂透皮给药制剂。通过油相滴定法制备了不同的 w/o 咖啡因纳米乳制剂。对热力学稳定的纳米乳进行了形态、粒径、粘度和折射率的特征描述。在 Franz 扩散池中使用大鼠皮肤作为渗透膜进行了体外皮肤渗透研究。将优化制剂的体外皮肤渗透曲线与咖啡因水溶液进行了比较。与咖啡因水溶液相比，纳米乳制剂的渗透参数显著增加（P<0.05）。优化的纳米乳制剂（C12）的稳态通量（J(ss)）和渗透系数（K(p)）分别为 147.55+/-8.21 microg/cm(2)/h 和 1.475 x 10(-2)+/-0.031 x 10(-2)cm/h。与其他制剂相比，优化制剂 C12 的增强比（E(r)）为 17.37。总的来说，这些结果表明 w/o 纳米乳是咖啡因经皮传递的良好载体。
