Kreilgaard Mads
Department of Neurochemistry and Discovery ADME, H Lundbeck A/S, Ottiliavej 9, DK-2500, Valby, Denmark.
Adv Drug Deliv Rev. 2002 Nov 1;54 Suppl 1:S77-98. doi: 10.1016/s0169-409x(02)00116-3.
In attempt to increase cutaneous drug delivery, microemulsion vehicles have been more and more frequently employed over recent years. Microemulsion formulations have been shown to be superior for both transdermal and dermal delivery of particularly lipophilic compounds, but also hydrophilic compounds appear to benefit from application in microemulsions compared to conventional vehicles, like hydrogels, emulsions and liposomes. The favourable drug delivery properties of microemulsions appear to mainly be attributed to the excellent solubility properties. However, the vehicles may also act as penetration enhancers depending on the oil/surfactant constituents, which involves a risk of inducing local irritancy. The correlation between microemulsion structure/composition and drug delivery potential is not yet fully elucidated. However, a few studies have indicated that the internal structure of microemulsions should allow free diffusion of the drug to optimise cutaneous delivery from these vehicles.
近年来,为了提高皮肤给药量,微乳剂载体的使用越来越频繁。微乳剂配方已被证明在特别是亲脂性化合物的透皮和真皮给药方面具有优势,而且与传统载体(如水凝胶、乳剂和脂质体)相比,亲水性化合物似乎也能从微乳剂的应用中受益。微乳剂良好的药物递送特性似乎主要归因于其出色的溶解性。然而,根据油/表面活性剂成分的不同,这些载体也可能充当渗透促进剂,这存在引起局部刺激的风险。微乳剂结构/组成与药物递送潜力之间的相关性尚未完全阐明。然而,一些研究表明,微乳剂的内部结构应允许药物自由扩散,以优化这些载体的皮肤给药效果。