In vitro evaluation of patch formulations for topical delivery of gentisic acid in rats.
In vitro evaluation of patch formulations for topical delivery of gentisic acid in rats.
复制标题
大鼠局部递送龙胆酸的贴剂制剂的体外评价。
DOI：
10.1016/s0928-0987(02)00255-5
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发表时间：
2003
期刊：
影响因子：
--
通讯作者：
Dae
中科院分区：
文献类型：
--
作者：
S. Bian;H. Doh;Jun;Jung Sun Kim;Chi;Dae
龙胆酸 (GA) 在化妆品中用作皮肤美白剂，通过抑制黑素体酪氨酸酶活性来影响黑色素的合成，从而治疗皮肤色素紊乱。为了实现GA有效局部递送至皮肤活性位点，开发了基质型透皮递送系统。在大鼠中研究了 GA 的体外皮肤渗透和皮肤沉积。在测试的五种压敏粘合剂中，DuroTak 87-2510 最有效地实现了最高的 GA 渗透率。在测试的增强剂中，十二胺表现出最有效的增强作用，当 DuroTak 87-2510 中掺入 6% GA 时，在 1% 浓度下，GA 的渗透速率显着提高至 112.99 (±30.12) μg/cm2/h。此外，GA的皮肤渗透速率与渗透12小时后皮肤沉积量之间观察到线性关系（r2=0.95）。因此，体外皮肤渗透数据可能有助于确定 GA 实际沉积在皮肤中的量。
Gentisic acid (GA) is used in cosmetics as a skin-whitening agent for the treatment of skin pigmentary disorders by influencing the synthesis of melanin through inhibition of melanosomal tyrosinase activity. In order to achieve effective topical delivery of GA to the active site in the skin, a matrix-type transdermal delivery system was developed. The in vitro skin permeation as well as skin deposition of GA was studied in rats. Among the five pressure-sensitive adhesives tested, DuroTak 87-2510 was the most effective to achieve the highest permeation rate of GA. Dodecylamine showed the most potent enhancement among the enhancers tested, and significantly increased the permeation rate of GA up to 112.99 (±30.12) μg/cm2per h at the concentration of 1%, when 6% GA was incorporated in DuroTak 87-2510. Moreover, a linear relationship was observed between the skin permeation rate of GA and the amount of the skin deposition after 12 h of permeation (r2=0.95). Thus, the in vitro skin permeation data may be useful to determine the amount of GA actually deposited in the skin.
影响因子：
5.8
作者：
Curto, EV;Kwong, C;Dooley, TP
通讯作者：
Dooley, TP