School of Medicine, Fu Jen Catholic University, Taipei County, Taiwan, China.
Acta Pharmacol Sin. 2010 Jan;31(1):118-26. doi: 10.1038/aps.2009.186. Epub 2009 Dec 21.
Silibinin (SB), silydianin (SD), and silychristin (SC) are components of silymarin. These compounds can be used to protect the skin from oxidative stress induced by ultraviolet (UV) irradiation and treat it. To this end, the absorption of silymarin constituents via the skin was examined in the present report.
Transport of SB, SD, and SC under the same thermodynamic activity through and into the skin and the effects of pH were studied in vitro using a Franz diffusion assembly.
The lipophilicity increased in the order of SC<SD<SB. Increased lipophilicity of a compound resulted in higher skin deposition but had a minor effect on permeation across the skin in the less-ionized form (pH 8). It is apparent that compounds in the less-ionized form showed higher skin uptake compared to the more-ionized form. Hyperproliferative skin produced by UVB exposure showed increased permeation of silymarin constituents in the less-ionized form, but it did not affect deposition within the skin. With in vivo topical application for 4 and 8 h, the skin deposition of SB was higher than those of SD and SC by 3.5 approximately 4.0- and 30 approximately 40-fold, respectively. The skin disruption and erythema test demonstrated that the topical application of these compounds for up to 24 h caused no apparent skin irritation.
The basic profiles of silymarin permeation via skin route were established.
水飞蓟宾（SB）、水飞蓟宁（SD）和水飞蓟亭（SC）是水飞蓟素的组成部分。这些化合物可用于保护皮肤免受紫外线（UV）照射引起的氧化应激，并对其进行治疗。为此，本报告研究了水飞蓟素成分通过皮肤的吸收。
使用 Franz 扩散组件，在体外研究了 SB、SD 和 SC 在相同热力学活性下通过皮肤和 pH 值对皮肤的传输。
亲脂性按 SC<SD<SB 的顺序增加。化合物的亲脂性增加导致皮肤沉积增加，但对较少电离形式（pH8）的皮肤透过性影响较小。显然，较少电离形式的化合物比更多电离形式的化合物具有更高的皮肤摄取率。UVB 照射产生的过度增生皮肤增加了水飞蓟素成分在较少电离形式下的渗透，但不影响皮肤内的沉积。在体内局部应用 4 和 8 h 后，SB 的皮肤沉积量分别比 SD 和 SC 高 3.5 至 4.0 倍和 30 至 40 倍。皮肤破坏和红斑试验表明，这些化合物的局部应用长达 24 h 不会引起明显的皮肤刺激。
确立了水飞蓟素经皮途径渗透的基本概况。
