Ho Suzanna, Calder Richard J, Thomas Christopher P, Heard Charles M
Welsh School of Pharmacy, Cardiff University, CF10 3XF, UK.
J Pharm Pharmacol. 2004 Nov;56(11):1357-64. doi: 10.1211/0022357044599.
The objective of this study was to examine the effects of ethanol and 1,8-cineole on the transcutaneous delivery of tamoxifen and gamma-linolenic acid (GLA) as a two-pronged anti-breast cancer therapy. Formulations containing tamoxifen and varying concentrations of borage oil (approximately 25% GLA), 1,8-cineole and ethanol were prepared and the simultaneous permeation of tamoxifen and GLA determined across full-thickness pig skin using Franz-type diffusion cells over 48 h. Analysis of tamoxifen and GLA (as methyl ester) were by reverse-phase HPLC. The highest flux of tamoxifen of 488.2 +/- 191 x 10(-3) microg cm(-2) h(-1) was observed with a formulation containing 20% 1,8-cineole and 20% ethanol. The same formulation also provided the greatest flux of GLA, 830.6 x 10(-3) microg cm(-2 )h(-1). The findings from this work demonstrate the ability of 1,8-cineole and ethanol to enhance the in-vitro permeation of tamoxifen and GLA across the skin and support the plausibility of simultaneously delivering tamoxifen and GLA transcutaneously as a two-pronged anti-breast cancer system.
本研究的目的是考察乙醇和1,8-桉叶素对他莫昔芬和γ-亚麻酸（GLA）经皮递送的影响，作为一种双管齐下的抗乳腺癌疗法。制备了含有他莫昔芬和不同浓度琉璃苣油（约25% GLA）、1,8-桉叶素和乙醇的制剂，并使用Franz型扩散池在48小时内测定了他莫昔芬和GLA在全层猪皮上的同步渗透情况。通过反相高效液相色谱法分析他莫昔芬和GLA（作为甲酯）。在含有20% 1,8-桉叶素和20%乙醇的制剂中观察到他莫昔芬的最高通量为488.2 +/- 191 x 10(-3) 微克·厘米(-2)·小时(-1)。同一制剂也提供了最大的GLA通量，即830.6 x 10(-3) 微克·厘米(-2)·小时(-1)。这项工作的研究结果表明，1,8-桉叶素和乙醇能够增强他莫昔芬和GLA在体外透过皮肤的渗透，并支持将他莫昔芬和GLA经皮同时递送作为双管齐下的抗乳腺癌系统的合理性。
