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含迷迭香酸载药纳米乳的水凝胶的制备、理化性质表征及体外研究。

Development, physico-chemical characterization and in-vitro studies of hydrogels containing rosmarinic acid-loaded nanoemulsion for topical application.

机构信息

Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.

Programa de Pós-Graduação em Biociências, Universidade Federal de Ciências da Saúde de Porto Alegre, Porto Alegre, RS, Brazil.

出版信息

J Pharm Pharmacol. 2019 Aug;71(8):1199-1208. doi: 10.1111/jphp.13102. Epub 2019 May 24.

Abstract

OBJECTIVES

Natural sources with antioxidant activity, such as rosmarinic acid (RA), have been considered as an interesting approach for the development of new anti-ageing skin products. In this context, this study aimed to develop hydrogels containing RA-loaded nanoemulsions and evaluate the effect of the addition of Tween 80 (a nonionic cosurfactant) in formulations intended to be used for topical application.

METHODS

Physico-chemical characterization, in-vitro release and skin retention/permeation from hydrogels of RA-loaded nanoemulsions (containing or not Tween 80) were evaluated. The RA-loaded nanoemulsion safety profiles were also investigated in keratinocytes (HaCaT cells).

KEY FINDINGS

It was observed that all formulations presented adequate physico-chemical characterization for topical application. Furthermore, the results also demonstrated that the presence of Tween 80 decreased the droplet size and polydispersity index of nanoemulsions and hydrogels. An extended RA release was noted for the hydrogels. However, when comparing the hydrogels, a positive effect of the presence of Tween 80 on RA retention/permeation in total skin was seen. The RA-loaded nanoemulsion safety profiles demonstrated a good tolerability (3.125-100 μm) in HaCaT cells.

CONCLUSIONS

The overall results demonstrated that the formulations developed in this study can be considered as a suitable carrier for RA in a topical application targeting new anti-ageing skin care products.

摘要

目的

具有抗氧化活性的天然物质,如迷迭香酸(RA),已被认为是开发新型抗衰老皮肤产品的一种有趣方法。在这种情况下,本研究旨在开发含有 RA 负载纳米乳液的水凝胶,并评估添加非离子型助表面活性剂吐温 80(Tween 80)对拟用于局部应用的制剂的影响。

方法

评估了载有 RA 的纳米乳液(含有或不含有 Tween 80)的水凝胶的物理化学特性、体外释放和皮肤保留/渗透。还研究了 RA 负载纳米乳液在角质细胞(HaCaT 细胞)中的安全性特征。

主要发现

所有制剂均具有适合局部应用的适当物理化学特性。此外,结果还表明,Tween 80 的存在降低了纳米乳液和水凝胶的粒径和多分散指数。水凝胶中 RA 的释放时间延长。然而,在比较水凝胶时,发现 Tween 80 的存在对总皮肤中 RA 的保留/渗透具有积极影响。RA 负载的纳米乳液安全性特征在 HaCaT 细胞中表现出良好的耐受性(3.125-100μm)。

结论

总的来说,研究结果表明,本研究中开发的制剂可被视为局部应用中 RA 的合适载体,旨在开发新型抗衰老皮肤护理产品。

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