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β-环糊精对常用优色林®防晒剂经皮吸收的影响。

The effect of Beta-cyclodextrin on percutaneous absorption of commonly used Eusolex® sunscreens.

作者信息

Shokri J, Hasanzadeh D, Ghanbarzadeh S, Dizadji-Ilkhchi M, Adibkia K

机构信息

Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.

出版信息

Drug Res (Stuttg). 2013 Nov;63(11):591-6. doi: 10.1055/s-0033-1349089. Epub 2013 Jul 10.

Abstract

BACKGROUND

There is a serious concern about the topical and systemic absorption of organic ultraviolet filters in sunscreen formulations and subsequent phototoxic and photo allergic reactions. Ideally, a sunscreen should localize in the surface of stratum corneum and create a barrier against UV radiation, but not penetrate into the underlying viable tissues and systemic circulation.

PURPOSE

The objective of the present study was to determine the effects of β-cyclodextrin (β-CDX) complexation on the transdermal penetration of 3 commonly used sun blocking agents, Eusolex ® 4360 (avobenzone), Eusolex ® 9020 (Oxybenzone) and Eusolex ® 232 (Ensulizole).

METHODS

The complexation of the sunscreen agents with β-CDX was performed by 3 methods and confirmed by differential scanning calorimetry (DSC). Sunscreens, and their physical mixtures and complexes with β-CDX were introduced into a model cream base (o/w emulsion). To find out the influence of β-CDX, sunscreen creams were applied to the rat skin in vitro in standard Franz diffusion cells and the amount of sunscreen permeated after 6 h was assessed by HPLC.

RESULTS

The skin penetration flux of the UV filters was significantly reduced (4–15 fold) by complexation with β-CDX. Complexation also could prolong absorption lag time of sun blocking agents to more than 150 min.

CONCLUSION

Considering the ability of β-CDX complexation in the reduction of flux and enhancement ratio as well as prolongation of absorption lag time, this technique could be very helpful for reducing systemic absorption of the UV filters and subsequent toxicity and allergic reaction.

摘要

背景

防晒配方中有机紫外线过滤剂的局部和全身吸收以及随后的光毒性和光过敏反应令人严重担忧。理想情况下,防晒霜应定位在角质层表面并形成抵御紫外线辐射的屏障,但不应渗透到下方的活组织和全身循环中。

目的

本研究的目的是确定β-环糊精(β-CDX)络合对3种常用防晒剂Eusolex®4360(阿伏苯宗)、Eusolex®9020(氧苯酮)和Eusolex®232(恩索利唑)经皮渗透的影响。

方法

通过3种方法进行防晒剂与β-CDX的络合,并通过差示扫描量热法(DSC)进行确认。将防晒霜及其与β-CDX的物理混合物和络合物引入模型乳膏基质(水包油乳液)中。为了了解β-CDX的影响,将防晒霜乳膏在标准Franz扩散池中体外应用于大鼠皮肤,并通过高效液相色谱法评估6小时后渗透的防晒剂含量。

结果

与β-CDX络合后,紫外线过滤剂的皮肤渗透通量显著降低(4至15倍)。络合还可将防晒剂的吸收滞后时间延长至150分钟以上。

结论

考虑到β-CDX络合在降低通量、提高增强率以及延长吸收滞后时间方面的能力,该技术可能对减少紫外线过滤剂的全身吸收以及随后的毒性和过敏反应非常有帮助。

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