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来自其磷脂复合物的黑芥子硫苷的体外皮肤渗透

In vitro skin permeation of sinigrin from its phytosome complex.

作者信息

Mazumder Anisha, Dwivedi Anupma, Fox Lizelle T, Brümmer Alicia, du Preez Jan L, Gerber Minja, du Plessis Jeanetta

机构信息

Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.

出版信息

J Pharm Pharmacol. 2016 Dec;68(12):1577-1583. doi: 10.1111/jphp.12594. Epub 2016 Oct 2.

Abstract

OBJECTIVES

Sinigrin is a major glucosinolate present in plants of the Brassicaceae family. Recently, sinigrin and its phytosome formulations have been investigated for its wound-healing actions, by our research group. The aim of this study was to demonstrate sinigrin drug release from its phytosome complex and also to determine whether the phytosome complex enhances the delivery of sinigrin into the skin when compared to free sinigrin.

METHODS

In vitro Franz cell diffusion studies were performed on human abdominal skin. The morphology of the phytosome complex was examined by transmission electron microscopy. The in vitro drug release was determined using dialysis sacks.

KEY FINDINGS

The in vitro drug release indicated a controlled and sustained release of sinigrin from the phytosome complex. Tape stripping results showed that the sinigrin-phytosome complex (0.5155 μg/ml) statistically significantly enhanced the delivery of sinigrin into the stratum corneum-epidermis when compared to the free sinigrin (0.0730 μg/ml).

CONCLUSIONS

These results suggested the possibility of utilizing sinigrin-phytosome complex, to optimally deliver sinigrin to the skin which can be further used for various skin-related diseases including wound healing.

摘要

目的

黑芥子硫苷是十字花科植物中存在的一种主要硫代葡萄糖苷。最近,我们的研究小组对黑芥子硫苷及其磷脂复合物的伤口愈合作用进行了研究。本研究的目的是证明黑芥子硫苷从其磷脂复合物中的药物释放情况,并确定与游离黑芥子硫苷相比,磷脂复合物是否能增强黑芥子硫苷向皮肤中的递送。

方法

在人腹部皮肤上进行体外弗兰兹细胞扩散研究。通过透射电子显微镜检查磷脂复合物的形态。使用透析袋测定体外药物释放情况。

主要发现

体外药物释放表明黑芥子硫苷从磷脂复合物中呈可控的持续释放。胶带剥离结果显示,与游离黑芥子硫苷(0.0730μg/ml)相比,黑芥子硫苷 - 磷脂复合物(0.5155μg/ml)在统计学上显著增强了黑芥子硫苷向角质层 - 表皮中的递送。

结论

这些结果表明利用黑芥子硫苷 - 磷脂复合物将黑芥子硫苷最佳递送至皮肤的可能性,这可进一步用于包括伤口愈合在内的各种皮肤相关疾病。

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