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防晒剂4-甲基亚苄基樟脑与环糊精的络合作用:对光稳定性和人体角质层渗透性的影响

Complexation of the sunscreen agent, 4-methylbenzylidene camphor with cyclodextrins: effect on photostability and human stratum corneum penetration.

作者信息

Scalia Santo, Tursilli Rosanna, Iannuccelli Valentina

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, via Fossato di Mortara 17, 44100 Ferrara, Italy.

出版信息

J Pharm Biomed Anal. 2007 May 9;44(1):29-34. doi: 10.1016/j.jpba.2007.01.016. Epub 2007 Jan 16.


DOI:10.1016/j.jpba.2007.01.016
PMID:17291707
Abstract

The interaction between the sunscreen agent, 4-methylbenzylidene camphor (4-MBC) and hydrophilic alpha-, beta- and gamma-cyclodextrin derivatives was investigated in water by phase-solubility analysis. Among the studied cyclodextrins, random methyl-beta-cyclodextrin (RM-beta-CD) had the greatest solubilizing activity. The complexation of the sunscreen agent with RM-beta-CD was confirmed by nuclear magnetic resonance spectroscopy and powder X-ray diffractometry. The light-induced decomposition of 4-MBC in emulsion vehicles was markedly decreased by complexation with RM-beta-CD (the extent of degradation, determined by HPLC, was 7.1% for the complex compared to 21.1% for free 4-MBC). The influence of RM-beta-CD on the human skin penetration of the sunscreen was investigated in vivo using the tape stripping method, a useful procedure for selectively removing the outermost cutaneous layers. Considerable quantities (21.2-25.1% of the applied dose) of 4-MBC permeated in the stratum corneum. However, no significant differences in the amounts of UV filter in the 10 first strips of the horny layer were observed between the formulations containing 4-MBC free or complexed with RM-beta-CD. Therefore, RM-beta-CD complexation did not alter the retention of 4-MBC in the superficial layers of the stratum corneum, where its action is more desirable.

摘要

通过相溶解度分析,在水中研究了防晒剂4-甲基亚苄基樟脑(4-MBC)与亲水性α-、β-和γ-环糊精衍生物之间的相互作用。在所研究的环糊精中,随机甲基-β-环糊精(RM-β-CD)具有最大的增溶活性。通过核磁共振光谱和粉末X射线衍射法证实了防晒剂与RM-β-CD的络合。与RM-β-CD络合可显著降低乳液载体中4-MBC的光致分解(通过高效液相色谱法测定,络合物的降解程度为7.1%,而游离4-MBC为21.1%)。使用胶带剥离法在体内研究了RM-β-CD对防晒剂经人体皮肤渗透的影响,胶带剥离法是一种选择性去除最外层皮肤层的有用方法。相当数量(占给药剂量的21.2-25.1%)的4-MBC渗透进入角质层。然而,在含有游离4-MBC或与RM-β-CD络合的制剂之间,在角质层的前10条胶带中未观察到紫外线过滤剂含量的显著差异。因此,RM-β-CD络合不会改变4-MBC在角质层表层的保留情况,而在角质层表层其作用更理想。

相似文献

[1]
Complexation of the sunscreen agent, 4-methylbenzylidene camphor with cyclodextrins: effect on photostability and human stratum corneum penetration.

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[2]
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[3]
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[2]
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[3]
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[4]
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[5]
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[6]
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[7]
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