Akomeah Franklin K, Martin Gary P, Muddle Andy G, Brown Marc B
Pharmaceutical Sciences Research Division, Kings College, London, United Kingdom.
Eur J Pharm Biopharm. 2008 Mar;68(3):724-34. doi: 10.1016/j.ejpb.2007.06.005. Epub 2007 Jun 14.
A transient reduction in the barrier nature of the skin can be a pre-requisite for successful (trans)dermal delivery of some drugs. The aim of this present study was to investigate and effect of a dermal abrading "rotating brush" device on percutaneous absorption and skin integrity. In vitro experiments were conducted using excised human epidermal membrane. The effect of device parameters (bristle type, treatment duration and applied pressure) on skin permeability of model solutes (methyl paraben, butyl paraben, caffeine, acyclovir and angiotensin II) with varying physicochemical properties was examined and compared to established methods of skin penetration enhancement (positive controls). The device parameter which was found to have the most marked effect on permeability of the compounds was bristle type. Profound changes (2- to 100-fold increase) were observed in the epidermal permeability of the hydrophilic penetrants (caffeine, acyclovir and angiotensin II), when the brush device was employed compared to positive controls (ethanol enhancement, delipidisation, iontophoresis and tape-stripping). Findings from this present study support the effectiveness of a rotating brush applied to the skin in enhancing epidermal permeability. Further optimization of operational parameters is required to exploit this simple and effective delivery device.
皮肤屏障性质的短暂降低可能是某些药物成功经皮给药的先决条件。本研究的目的是研究一种皮肤磨损“旋转刷”装置对经皮吸收和皮肤完整性的影响。使用切除的人表皮膜进行体外实验。研究了装置参数（刷毛类型、处理持续时间和施加压力）对具有不同理化性质的模型溶质（对羟基苯甲酸甲酯、对羟基苯甲酸丁酯、咖啡因、阿昔洛韦和血管紧张素II）皮肤渗透性的影响，并与已确立的皮肤渗透增强方法（阳性对照）进行比较。发现对化合物渗透性影响最显著的装置参数是刷毛类型。与阳性对照（乙醇增强、脱脂、离子导入和胶带剥离）相比，当使用刷式装置时，亲水性渗透剂（咖啡因、阿昔洛韦和血管紧张素II）的表皮渗透性出现了显著变化（增加2至100倍）。本研究结果支持将旋转刷应用于皮肤可增强表皮渗透性的有效性。需要进一步优化操作参数以利用这种简单有效的给药装置。
