Influence of cyclodextrins on in vitro human skin absorption of the sunscreen, butyl-methoxydibenzoylmethane

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摘要：

The effects of hydroxypropyl-β-cyclodextrin (HP-β-CD) and sulfobutylether-β-CD (SBE7-β-CD) on in vitro human skin penetration and retention of the sunscreen agent butyl-methoxydibenzoylmethane (BM-DBM) were investigated. The interaction between the UV filter and the cyclodextrins was studied in water by phase-solubility analysis. Solid complexes were prepared by the co-evaporation method and characterized by 1H NMR spectroscopy, thermal analysis and powder X-ray diffraction. Solutions containing BM-DBM free or complexed with cyclodextrins were applied to excised human skin in Franz diffusion cells and the amount of sunscreen permeated after 6 h into the stratum corneum, viable epidermis, dermis and receptor fluid was assessed by HPLC. As much as 14.10–16.78% of the applied dose of BM-DBM penetrated within the skin tissue. No sunscreen was detected in the dermis and in the receiver phase. The greater proportion (84.6–95.5%) of the absorbed UV filter was localized in the stratum corneum with no significant differences between uncomplexed or complexed BM-DBM. Notable levels (2.29% of the applied dose) of the sunscreen agent accumulated in the epidermis from the preparation containing free BM-DBM. The epidermal concentration of the UV filter was markedly reduced (0.66% of the applied dose) by complexation with SBE7-β-CD, whereas HP-β-CD had no effect. The decreased BM-DBM retention in the epidermal region achieved by SBE7-β-CD limits direct contact of the sunscreen and of its reactive photolytic products with the skin viable tissues.

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关键词：

Sunscreen agent Butyl-methoxydibenzoylmethane Cyclodextrin Complexation Human skin Percutaneous penetration

DOI：

10.1016/j.ijpharm.2004.05.021

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年份：

2004