Influence of hydroxypropyl-β-cyclodextrin on the transdermal permeation and skin accumulation of oxybenzone

被引:33
|
作者
Felton, LA [1 ]
Wiley, CJ [1 ]
Godwin, DA [1 ]
机构
[1] Univ New Mexico, Hlth Sci Ctr, Coll Pharm, Albuquerque, NM 87131 USA
关键词
complexation; hydroxypropyl-beta-cyclodextrin; oxybenzone; reservoir; skin accumulation; transdermal permeation;
D O I
10.1081/DDC-120014578
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The objective of the present studs eras to determine the effects of hydroxypropyl-beta-cyclodextrin (HPCD) concentration on the transdermal permeation and skin accumulation of a model ultraviolet (UV) absorber, oxybenzone. The concentration of oxybenzone was held constant at 2.67 mg/mL for all formulations, while the HPCD concentrations varied from 0 to 20 (w/w). Complexation of oxybenzone by HPCD was demonstrated by differential scanning calorimetry. A modified Franz cell apparatus eras used in the transdermal experiments, with aliquots of the receptor fluid assayed for oxybenzone by high-performance liquid chromatography. Front the permeation data, flux of the drug eras calculated. Skins mere removed from the diffusion cells at specified time points ores a 24-hr period and the oxybenzone content in the skin determined. The aqueous solubility of oxybenzone increased linearly with increasing HPCD concentration, following a Higuchi A(L)-type complexation. The stability constant of the reaction was calculated from the phase-solubility diagram and found to be 2047 M-1. As the concentration of HPCD eras increased from 0 to 10%, transdermal permeation and shin accumulation of oxybenzone increased. Maximum flux occurred at 10% HPCD, where sufficient cyclodextrin eras added to completely solubilize all oxybenzone. When the concentration of HPCD was increased to 20%, both transdermal permeation and skin accumulation decreased. These data suggest the formation of a drug reservoir on the surface of the skin.
引用
收藏
页码:1117 / 1124
页数:8
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