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评价包含在防晒霜中的辛基对甲氧基肉桂酸酯的脂质体和环糊精:制剂、特性和体外渗透研究。

Evaluation of octyl p-methoxycinnamate included in liposomes and cyclodextrins in anti-solar preparations: preparations, characterizations and in vitro penetration studies.

机构信息

Medicines Department, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil.

出版信息

Int J Nanomedicine. 2012;7:3045-58. doi: 10.2147/IJN.S28550. Epub 2012 Jun 20.

Abstract

PURPOSE

Awareness of the harmful effects of ultraviolet radiation has led to the increasing use of sunscreens, thus, the development of safe and effective antisolar preparations is important. The inclusion of sunscreen molecules in different release systems, like liposomes (lipo) and cyclodextrins (CD) is therefore required.

METHODS

The in vivo sun protection factor (SPF), water resistance, and in vitro transdermal penetration test of octyl p-methoxycinnamate (OMC) in different dispersions, such as OMC encapsulated in liposomes (lipo/OMC), OMC encapsulated in β-cyclodextrins (β-CD/OMC), OMC encapsulated in both release systems (lipo/OMC and β-CD/OMC), and an OMC-free formulation were determined.

RESULTS

Although the formulation containing only the lipo/OMC system revealed high value of in vivo SPF (11.0 ± 1.3) and water resistance (SPF = 10.3 ± 2.2), the formulation containing both release systems (lipo/OMC + β-cyclodextrin/OMC) showed the best result in the in vivo SPF test (11.6 ± 1.6). In the penetration test, the formulation containing the lipo/OMC system had better performance, since a high amount of OMC in the epidermis (18.04 ± 1.17 μg) and a low amount of OMC in the dermis (9.4 ± 2.36 μg) were observed. These results suggest that liposomes interact with the cells of the stratum corneum, promoting retention of OMC in this layer.

CONCLUSION

According to our study, the lipo/OMC system is the most advantageous release system, due to its ability to both increase the amount of OMC in the epidermis and decrease the risk of percutaneous absorption.

摘要

目的

由于人们意识到紫外线辐射的有害影响,防晒霜的使用越来越多,因此开发安全有效的防晒制剂非常重要。因此,需要将防晒分子纳入不同的释放系统,如脂质体(lipo)和环糊精(CD)。

方法

在不同的分散体中,测定了辛基甲氧基肉桂酸酯(OMC)的体内防晒因子(SPF)、耐水性和体外透皮渗透试验,如包裹在脂质体中的 OMC(lipo/OMC)、包裹在β-环糊精中的 OMC(β-CD/OMC)、同时包裹在两种释放系统中的 OMC(lipo/OMC 和β-CD/OMC)和不含 OMC 的制剂。

结果

虽然仅包含 lipo/OMC 系统的制剂显示出高的体内 SPF 值(11.0 ± 1.3)和耐水性(SPF = 10.3 ± 2.2),但包含两种释放系统的制剂(lipo/OMC +β-环糊精/OMC)在体内 SPF 测试中显示出最佳结果(11.6 ± 1.6)。在渗透试验中,包含 lipo/OMC 系统的制剂表现出更好的性能,因为在表皮中观察到大量的 OMC(18.04 ± 1.17 μg)和在真皮中观察到低量的 OMC(9.4 ± 2.36 μg)。这些结果表明,脂质体与角质层细胞相互作用,促进 OMC 在该层中的保留。

结论

根据我们的研究,lipo/OMC 系统是最有利的释放系统,因为它既能增加表皮中 OMC 的含量,又能降低经皮吸收的风险。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e468/3391002/e72e1a3b00d9/ijn-7-3045f1.jpg

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