Kear Clifford L, Yang Jing, Godwin Donald A, Felton Linda A
College of Pharmacy, University of New Mexico, Albuquerque, New Mexico 87131, USA.
Drug Dev Ind Pharm. 2008 Jul;34(7):692-7. doi: 10.1080/03639040701842428.
The objective of this study was to investigate the mechanism by which hydroxypropyl-beta-cyclodextrin (HPCD) increases transdermal permeation. Hairless mouse skin was pretreated with HPCD solutions for up to 4 h. After removing the HPCD, corticosteroid-containing suspensions were applied and the transdermal flux and skin accumulation of two model drugs were investigated. After pretreatment, changes to the stratum corneum endothermic melting transitions were determined as an indication of HPCD-induced lipid disorganization. Results demonstrated that HPCD pretreatment had no significant effect on the transdermal permeation or skin accumulation of the model corticosteroids. These findings suggest that HPCD functions to enhance the apparent solubility of the drug in the formulation, thus increasing transdermal permeation rather than extracting lipids from the skin.
本研究的目的是探究羟丙基-β-环糊精(HPCD)增加透皮渗透的机制。用HPCD溶液对无毛小鼠皮肤进行长达4小时的预处理。去除HPCD后,应用含皮质类固醇的混悬液,并研究两种模型药物的透皮通量和皮肤蓄积情况。预处理后,测定角质层吸热熔融转变的变化,以表明HPCD诱导的脂质紊乱。结果表明,HPCD预处理对模型皮质类固醇的透皮渗透或皮肤蓄积没有显著影响。这些发现表明,HPCD的作用是提高药物在制剂中的表观溶解度,从而增加透皮渗透,而不是从皮肤中提取脂质。