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羟丙基-β-环糊精对阿伏苯宗透皮渗透及光稳定性的影响

Influence of hydroxypropyl-beta-cyclodextrin on transdermal penetration and photostability of avobenzone.

作者信息

Yang Jing, Wiley Cody J, Godwin Donald A, Felton Linda A

机构信息

University of New Mexico, Albuquerque, NM 87131, USA.

出版信息

Eur J Pharm Biopharm. 2008 Jun;69(2):605-12. doi: 10.1016/j.ejpb.2007.12.015. Epub 2007 Dec 25.

Abstract

The objective of the present study was to determine the effects of hydroxypropyl-beta-cyclodextrin (HPCD) complexation on the transdermal penetration and photostability of a model ultraviolet A (UVA) absorber, butyl methoxydibenzoylmethane (avobenzone), and to determine the influence of complexation on in vivo photoprotection. Avobenzone-HPCD complexation was demonstrated by differential scanning calorimetry. Formulations containing 0.12 mg/ml avobenzone and up to 30% (w/w) HPCD were prepared. Transdermal penetration was conducted using a modified Franz diffusion cell apparatus. As the concentration of HPCD was increased from 0% to 20%, transdermal permeation increased. Maximum flux occurred at 20% HPCD, where sufficient cyclodextrin was present to completely solubilize all avobenzone. When the concentration of HPCD was increased to 30%, transdermal penetration decreased, suggesting the formation of an avobenzone reservoir on the skin surface. Photostability of avobenzone was investigated under 100, 250, and 500 kJ/m2 UVA irradiation. The 30% HPCD formulation was the most photostable, followed by 20%, 10%, and 0% formulations. In vivo, the 30% HPCD formulation afforded the best photoprotection, as evidenced by the lowest extent of sunburn cell formation and edema induction. This work indicates that inclusion of HPCD in sunscreen formulations may enhance photoprotection by reducing both skin penetration and photodecomposition of UV absorbers.

摘要

本研究的目的是确定羟丙基-β-环糊精(HPCD)络合对模型紫外线A(UVA)吸收剂丁基甲氧基二苯甲酰甲烷(阿伏苯宗)经皮渗透和光稳定性的影响,并确定络合对体内光防护的影响。通过差示扫描量热法证明了阿伏苯宗与HPCD的络合。制备了含有0.12mg/ml阿伏苯宗和高达30%(w/w)HPCD的制剂。使用改良的Franz扩散池装置进行经皮渗透实验。随着HPCD浓度从0%增加到20%,经皮渗透增加。在HPCD浓度为20%时出现最大通量,此时存在足够的环糊精以完全溶解所有阿伏苯宗。当HPCD浓度增加到30%时,经皮渗透下降,表明在皮肤表面形成了阿伏苯宗储库。在100、250和500kJ/m2的UVA照射下研究了阿伏苯宗的光稳定性。30%HPCD制剂的光稳定性最高,其次是20%、10%和0%的制剂。在体内,30%HPCD制剂提供了最佳的光防护,晒伤细胞形成和水肿诱导程度最低证明了这一点。这项工作表明,在防晒制剂中加入HPCD可通过减少紫外线吸收剂的皮肤渗透和光分解来增强光防护。

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