Batchelder Rachel J, Calder Richard J, Thomas Chris P, Heard Charles M
Welsh School of Pharmacy, Cardiff University, Cardiff CF10 3XF, UK.
Int J Pharm. 2004 Sep 28;283(1-2):45-51. doi: 10.1016/j.ijpharm.2004.06.007.
The aim of this study was to investigate the feasibility of the transdermal delivery of catechins and caffeine from green tea extract. Drug-in-adhesive patches containing 1.35, 1.03, 0.68, and 0.32 mg cm(-2) green tea extract were formulated and the dissolution of (-)-epigallocatechin gallate (EGCg), (-)-epigallocatechin (EGC) and (-)-epicatechin (EC) from these was determined. Transdermal delivery was determined across full thickness pig ear skin from saturated solutions of green tea extract in pH 5.5 citrate-phosphate buffer, polyethylene glycol 400 and a 50:50 mixture of the citrate phosphate buffer and polyethylene glycol in addition to patches containing 1.35 mg cm(-2) green tea extract. Dissolution experiments indicated first order release which was dose dependent in respect of the loading level, although the amounts permeated were not always proportional to the amounts in the formulation. The highest percentage permeation of EGCg was found to be from the patch formulation. EGCg, EGC and EC were all successfully delivered transdermally from saturated solutions and adhesive patches containing green tea extract in this study. There was some evidence for the dermal metabolism of EGCg, but after 24 h 0.1% permeated from the patches containing 1.35 mg cm(-2) green tea extract. This was equivalent to the percentage absorbed after intragastric administration of green tea extract in rats. In addition, the concentration of EGCg in the Franz cell receptor chamber after 24 h permeation from the 0.9 cm diameter patch containing 1.35 mg cm(-2) was within the range of Cmax plasma levels achieved after oral dosing of 2.2-4.2 gm(-2) green tea extract. Caffeine was also delivered at concentrations above those previously reported.
本研究的目的是探究从绿茶提取物中经皮递送儿茶素和咖啡因的可行性。制备了含有1.35、1.03、0.68和0.32 mg/cm²绿茶提取物的贴剂,并测定了其中(-)-表没食子儿茶素没食子酸酯(EGCg)、(-)-表没食子儿茶素(EGC)和(-)-表儿茶素(EC)的溶出情况。除了含有1.35 mg/cm²绿茶提取物的贴剂外,还测定了绿茶提取物在pH 5.5的柠檬酸-磷酸盐缓冲液、聚乙二醇400以及柠檬酸磷酸盐缓冲液与聚乙二醇50:50混合物中的饱和溶液经猪耳全层皮肤的透皮递送情况。溶出实验表明释放符合一级动力学,且与载药量呈剂量依赖性,尽管渗透量并不总是与制剂中的含量成正比。发现EGCg从贴剂制剂中的渗透百分比最高。在本研究中,EGCg、EGC和EC均成功地从含有绿茶提取物的饱和溶液和贴剂经皮递送。有证据表明EGCg存在皮肤代谢,但24小时后,从含有1.35 mg/cm²绿茶提取物的贴剂中渗透出0.1%。这与大鼠胃内给予绿茶提取物后的吸收百分比相当。此外,从直径0.9 cm、含有1.35 mg/cm²的贴剂中渗透24小时后,Franz细胞受体室中EGCg的浓度在口服2.2 - 4.2 g/m²绿茶提取物后达到的血浆Cmax水平范围内。咖啡因也以高于先前报道的浓度递送。
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