抗氧化剂硒-L-蛋氨酸及其它硒形态的经皮体外和体内吸收。
In vitro and in vivo percutaneous absorption of seleno-L-methionine, an antioxidant agent, and other selenium species.
机构信息
Center for General Education, Chang Gung University of Science and Technology, Kweishan, Taoyuan, Taiwan, China.
出版信息
Acta Pharmacol Sin. 2011 Sep;32(9):1181-90. doi: 10.1038/aps.2011.89. Epub 2011 Jul 25.
AIM
To investigate the in vitro and in vivo percutaneous absorption of seleno-L-methionine (Se-L-M), an ultraviolet (UV)-protecting agent, from aqueous solutions.
METHODS
Aqueous solutions of Se-L-M were prepared in pH 4, 8, and 10.8 buffers. The pH 8 buffer contained 30% glycerol, propylene glycol (PG) and polyethylene glycol (PEG) 400. The in vitro skin permeation of Se-L-M via porcine skin and nude mouse skin was measured and compared using Franz diffusion cells. The in vivo skin tolerance study was performed, which examined transepidermal water loss (TEWL), skin pH and erythema.
RESULTS
In the excised porcine skin, the flux was 0.1, 11.4 and 8.2 μg·cm(-2)·h(-1) for the pH 4, 8, and 10.8 buffers, respectively. A linear correlation between the flux and skin deposition was determined. According to permeation across skin with different treatments (stripping, delipidation, and ethanol treatments), it was determined that the intracellular route comprised the predominant pathway for Se-L-M permeation from pH 8 buffer. Aqueous solutions of seleno-DL-methionine (Se-DL-M), selenium sulfide and selenium-containing quantum dot nanoparticles were also used as donor systems. The DL form showed a lower flux (7.0 vs 11.4 μg·cm(-2)·h(-1)) and skin uptake (23.4 vs 47.3 μg/g) as compared to the L form, indicating stereoselective permeation of this compound. There was no or only negligible permeation of selenium sulfide and quantum dots into and across the skin. With in vivo topical application for 4 and 8 h, the skin deposition of Se-L-M was about 7 μg/g, and values were comparable to each other. The topical application of Se-L-M for up to 5 d did not caused apparent skin irritation. However, slight inflammation of the dermis was noted according to the histopathological examination.
CONCLUSION
Se-L-M was readily absorbed by the skin in both the in vitro and in vivo experiments. The established profiles of Se-L-M skin absorption will be helpful in developing topical products of this compound.
目的
研究紫外线（UV）保护剂硒-L-蛋氨酸（Se-L-M）从水溶液中的体外和体内经皮吸收。
方法
在 pH 4、8 和 10.8 缓冲液中制备 Se-L-M 的水溶液。pH 8 缓冲液中含有 30%甘油、丙二醇（PG）和聚乙二醇（PEG）400。使用 Franz 扩散池测量并比较 Se-L-M 通过猪皮和裸鼠皮的体外皮肤渗透。进行了体内皮肤耐受性研究，检查经皮水分损失（TEWL）、皮肤 pH 值和红斑。
结果
在离体猪皮中，pH 4、8 和 10.8 缓冲液的通量分别为 0.1、11.4 和 8.2μg·cm(-2)·h(-1)。通量与皮肤沉积之间存在线性相关性。根据不同处理（剥离、脱脂和乙醇处理）透过皮肤的情况，确定细胞内途径是 Se-L-M 从 pH 8 缓冲液中渗透的主要途径。还将硒-DL-蛋氨酸（Se-DL-M）、硒硫化物和含硒量子点纳米粒子的水溶液用作供体系统。与 L 形式相比，DL 形式显示出较低的通量（7.0 与 11.4μg·cm(-2)·h(-1)）和皮肤摄取量（23.4 与 47.3μg/g），表明该化合物具有立体选择性渗透。硒硫化物和量子点几乎没有或只有轻微的渗透进入和穿过皮肤。在 4 和 8 h 的局部应用中，Se-L-M 的皮肤沉积量约为 7μg/g，彼此相当。Se-L-M 的局部应用长达 5 天不会引起明显的皮肤刺激。然而，根据组织病理学检查，真皮有轻微炎症。
结论
在体外和体内实验中，Se-L-M 很容易被皮肤吸收。所建立的 Se-L-M 皮肤吸收概况将有助于开发该化合物的局部产品。
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