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局部和经皮递送左旋肉碱。

Topical and transdermal delivery of L-carnitine.

机构信息

Unit for Drug Research and Development, North-West University, Potchefstroom, South Africa.

出版信息

Skin Pharmacol Physiol. 2011;24(6):330-6. doi: 10.1159/000330385. Epub 2011 Aug 11.

DOI:10.1159/000330385
PMID:21832865
Abstract

BACKGROUND

The two types of skin aging (intrinsic and extrinsic) share important molecular features, while having distinct differences on the macromolecular level: both lead to increased production of reactive oxygen species, enhanced matrix metalloproteinase expression and decreased procollagen synthesis. L-Carnitine L-tartrate has been reported to have anti-aging effects.

AIM AND METHODS

The delivery as well as the transport of L-carnitine to the target sites, i.e. stratum corneum and epidermis-dermis of female abdominal skin, with and without the use of Pheroid™ as delivery system, were investigated during this study by use of Franz diffusion cells and analysed by liquid chromatography/mass spectrometry. The presence of endogenous L-carnitine in human skin was also investigated.

RESULTS AND CONCLUSION

The Pheroid™ delivery system enhanced the diffusion of L-carnitine through the skin, although the phosphate buffer solution (PBS) showed a higher concentration of the active agent in the skin layers. This could be because Pheroid, being more lipophilic than PBS, improved the diffusion of L-carnitine through the skin layers, consequently leading to a lesser amount of L-carnitine delivered to the target site, i.e. the epidermis-dermis.

摘要

背景

两种类型的皮肤老化(内在的和外在的)具有重要的分子特征,而在大分子水平上有明显的区别:两者都导致活性氧的产生增加,基质金属蛋白酶表达增强,原胶原蛋白合成减少。L-肉碱酒石酸盐已被报道具有抗衰老作用。

目的和方法

本研究通过Franz 扩散池,使用液相色谱/质谱分析,考察了 L-肉碱在有和没有 Pheroid™ 作为递送系统的情况下,递送到女性腹部皮肤角质层和表皮-真皮靶部位的输送和转运情况。还研究了内源性 L-肉碱在人体皮肤中的存在情况。

结果和结论

Pheroid™ 递送系统增强了 L-肉碱通过皮肤的扩散,尽管磷酸盐缓冲液(PBS)显示皮肤层中活性物质的浓度更高。这可能是因为 Pheroid 比 PBS 更亲脂,从而改善了 L-肉碱通过皮肤层的扩散,因此导致递送到靶部位(即表皮-真皮)的 L-肉碱量减少。

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