El Maghraby G M, Williams A C
School of Pharmacy, University of Reading, Reading, Whiteknights, PO Box 226, Reading, RG66AP Berkshire, UK.
Expert Opin Drug Deliv. 2009 Feb;6(2):149-63. doi: 10.1517/17425240802691059.
The history of using vesicular systems for drug delivery to and through skin started nearly three decades ago with a study utilising phospholipid liposomes to improve skin deposition and reduce systemic effects of triamcinolone acetonide. Subsequently, many researchers evaluated liposomes with respect to skin delivery, with the majority of them recording localised effects and relatively few studies showing transdermal delivery effects. Shortly after this, transfersomes were developed with claims about their ability to deliver their payload into and through the skin with efficiencies similar to subcutaneous administration. Since these vesicles are ultradeformable, they were thought to penetrate intact skin deep enough to reach the systemic circulation. Their mechanisms of action remain controversial, with diverse processes being reported. Parallel to this development, other classes of vesicles were produced, with ethanol being included into the vesicles to provide flexibility (as in ethosomes); vesicles were constructed from surfactants and cholesterol (as in niosomes). The ultradeformable vesicles showed variable efficiency in delivering low-molecular-weight and macromolecular drugs. This article will critically evaluate vesicular systems for dermal and transdermal delivery of drugs, considering both their efficacy and their potential mechanisms of action.
利用囊泡系统将药物递送至皮肤并透过皮肤的历史始于近三十年前的一项研究，该研究利用磷脂脂质体来改善皮肤药物沉积并降低曲安奈德的全身效应。随后，许多研究人员对脂质体的皮肤递送进行了评估，其中大多数记录了局部效应，只有相对较少的研究显示出透皮递送效果。在此之后不久，传递体被开发出来，据称它们能够以与皮下给药相似的效率将其负载递送至皮肤内并透过皮肤。由于这些囊泡具有超变形性，人们认为它们能够穿透完整皮肤足够深以进入体循环。它们的作用机制仍存在争议，有多种过程被报道。与这一发展并行的是，还产生了其他类型的囊泡，将乙醇纳入囊泡以提供柔韧性（如醇质体）；囊泡由表面活性剂和胆固醇构建而成（如非离子型脂质体）。超变形囊泡在递送低分子量和大分子药物方面显示出不同的效率。本文将批判性地评估用于药物经皮和透皮递送的囊泡系统，同时考虑它们的疗效及其潜在的作用机制。
