Sinico Chiara, Fadda Anna Maria
University of Cagliari, Dipartimento Farmaco Chimico Tecnologico, 09124 Cagliari -Italy.
Expert Opin Drug Deliv. 2009 Aug;6(8):813-25. doi: 10.1517/17425240903071029.
The skin can offer several advantages as a route of drug administration although its barrier nature makes it difficult for most drugs to penetrate into and permeate through it. During the past decades there has been a lot of interest in lipid vesicles as a tool to improve drug topical delivery. Vesicular systems such as liposomes, niosomes, ethosomes and elastic, deformable vesicles provide an alternative for improved skin drug delivery. The function of vesicles as topical delivery systems is controversial with variable effects being reported in relation to the type of vesicles and their composition. In fact, vesicles can act as drug carriers controlling active release; they can provide a localized depot in the skin for dermally active compounds and enhance transdermal drug delivery. A wide variety of lipids and surfactants can be used to prepare vesicles, which are commonly composed of phospholipids (liposomes) or non-ionic surfactants (niosomes). Vesicle composition and preparation method influence their physicochemical properties (size, charge, lamellarity, thermodynamic state, deformability) and therefore their efficacy as drug delivery systems. A review of vesicle value in localizing drugs within the skin at the site of action will be provided with emphasis on their potential mechanism of action.
尽管皮肤的屏障特性使得大多数药物难以渗透进入和透过，但作为给药途径，皮肤具有若干优势。在过去几十年中，脂质囊泡作为改善药物局部递送的工具受到了广泛关注。脂质体、非离子型脂质体、醇质体和弹性可变形囊泡等囊泡系统为改善皮肤药物递送提供了一种替代方法。囊泡作为局部递送系统的功能存在争议，关于囊泡类型及其组成的报道显示出不同的效果。事实上，囊泡可作为控制药物活性释放的载体；它们可为皮肤活性化合物在皮肤中提供局部储库，并增强透皮药物递送。多种脂质和表面活性剂可用于制备囊泡，囊泡通常由磷脂（脂质体）或非离子表面活性剂（非离子型脂质体）组成。囊泡的组成和制备方法会影响其物理化学性质（大小、电荷、层数、热力学状态、可变形性），进而影响其作为药物递送系统的功效。本文将综述囊泡在将药物定位在皮肤作用部位方面的价值，并重点阐述其潜在作用机制。
