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纳米乳在石榴皮多酚经皮给药中的潜在应用。

Potential Application of Nanoemulsions for Skin Delivery of Pomegranate Peel Polyphenols.

机构信息

Programa de Pós-Graduação em Farmácia, Universidade Federal de Santa Catarina, Florianópolis, SC, 88040-970, Brazil.

Departamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal de Santa Catarina, Campus Universitário Trindade, Florianópolis, SC, 88040-900, Brazil.

出版信息

AAPS PharmSciTech. 2017 Nov;18(8):3307-3314. doi: 10.1208/s12249-017-0818-x. Epub 2017 Jun 8.

Abstract

Pomegranate peel and seeds have demonstrated to possess antioxidant compounds with potential application to protect the skin against the ultraviolet radiation damage. However, the photoprotection activity is dependent on the amount of these compounds that reach the viable skin layers. In this paper, we describe the in vitro skin permeation and retention of the major pomegranate peel polyphenols using Franz diffusion cells, after entrapping a ethyl acetate fraction (EAF) from Punica granatum peel extract into nanoemulsions (NEs) prepared with pomegranate seed oil (PSO) or medium chain triglyceride oil (MCT). The in vitro skin permeation of gallic acid (GA), ellagic acid (EA), and punicalagin (PC) was evaluated using a HPLC-DAD validated method. After 8 h of skin permeation, all polyphenol compounds were mostly retained in the skin and did not reach the receptor compartment. However, a 2.2-fold enhancement of the retained amount of gallic acid in the stratum corneum was verified after EAF-loaded NEs are applied, when compared with the free EAF. GA and EA were delivered to the viable epidermis and dermis only when nanoemulsions were applied onto the skin. The mean retained amounts of GA and EA in the EP and DE after applying the EAF-loaded PSO-NE were 1.78 and 1.36 μg cm and 1.10 and 0.97 μg cm, respectively. Similar values were obtained after applying the EAF-loaded MCT-NE. The skin permeation results were supported by the confocal microscopy images. These results evidenced the promising application of nanoemulsions to deliver the pomegranate polyphenols into the deeper skin layers.

摘要

石榴皮和种子已被证明含有具有抗氧化作用的化合物,具有保护皮肤免受紫外线辐射损伤的潜在应用。然而,光保护活性取决于到达有活力的皮肤层的这些化合物的量。在本文中,我们描述了使用Franz 扩散细胞将石榴皮提取物的乙酸乙酯部分(EAF)包封到由石榴籽油(PSO)或中链甘油三酯油(MCT)制备的纳米乳液(NE)中后,主要石榴皮多酚在体外皮肤中的渗透和保留。使用 HPLC-DAD 验证的方法评估了没食子酸(GA)、鞣花酸(EA)和安石榴甙(PC)的体外皮肤渗透。经过 8 小时的皮肤渗透,所有多酚化合物大部分都保留在皮肤中,没有到达受体隔室。然而,与游离 EAF 相比,在 EAF 负载的 NE 应用后,在角质层中 GA 的保留量增加了 2.2 倍。只有在纳米乳液应用于皮肤时,GA 和 EA 才被递送到有活力的表皮和真皮中。在应用 EAF 负载的 PSO-NE 后,GA 和 EA 在 EP 和 DE 中的平均保留量分别为 1.78 和 1.36μg·cm-2和 1.10 和 0.97μg·cm-2。应用 EAF 负载的 MCT-NE 后也得到了类似的值。皮肤渗透结果得到共聚焦显微镜图像的支持。这些结果证明了纳米乳液在将石榴多酚递送到更深的皮肤层中的有前途的应用。

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