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脂质体用于经皮给药的最新进展和展望。

Recent Advances and Perspectives in Liposomes for Cutaneous Drug Delivery.

机构信息

Medical Department, Federal University of Sao Paulo (UNIFESP), Sao Paulo, Brazil.

Drugs and Medicines Department, College of Pharmaceutical Sciences of Araraquara, Sao Paulo State University (UNESP), Sao Paulo, Brazil.

出版信息

Curr Med Chem. 2018 Feb 13;25(5):606-635. doi: 10.2174/0929867324666171009120154.

Abstract

The cutaneous route is attractive for the delivery of drugs in the treatment of a wide variety of diseases. However the stratum corneum (SC) is an effective barrier that hampers skin penetration. Within this context, liposomes emerge as a potential carrier for improving topical delivery of therapeutic agents. In this review, we aimed to discuss key aspects for the topical delivery by drug-loaded liposomes. Phospholipid type and phase transition temperature have been shown to affect liposomal topical delivery. The effect of surface charge is subject to considerable variation depending on drug and composition. In addition, modified vesicles with the presence of components for permeation enhancement, such as surfactants and solvents, have been shown to have a considerable effect. These liposomes include: Transfersomes, Niosomes, Ethosomes, Transethosomes, Invasomes, coated liposomes, penetration enhancer containing vesicles (PEVs), fatty acids vesicles, Archaeosomes and Marinosomes. Furthermore, adding polymeric coating onto liposome surface could influence cutaneous delivery. Mechanisms of delivery include intact vesicular skin penetration, free drug diffusion, permeation enhancement, vesicle adsorption to and/or fusion with the SC, trans-appendageal penetration, among others. Finally, several skin conditions, including acne, melasma, skin aging, fungal infections and skin cancer, have benefited from liposomal topical delivery of drugs, with promising in vitro and in vivo results. However, despite the existence of some clinical trials, more studies are needed to be conducted in order to explore the potential of liposomes in the dermatological field.

摘要

皮肤给药途径在治疗各种疾病的药物传递中具有吸引力。然而,角质层(SC)是一种有效的屏障,阻碍了皮肤渗透。在这种情况下,脂质体作为一种提高治疗剂局部递送的潜在载体出现。在这篇综述中,我们旨在讨论载药脂质体进行局部递送的关键方面。已经表明,磷脂类型和相转变温度会影响脂质体的局部递送。表面电荷的影响取决于药物和组成的变化。此外,具有增强渗透成分(如表面活性剂和溶剂)的改性囊泡已被证明具有相当大的作用。这些脂质体包括:传递体、尼奥斯omes、醇质体、转醇质体、侵入体、包被脂质体、包含渗透增强剂的囊泡(PEVs)、脂肪酸囊泡、Archaeosomes 和 Marinosomes。此外,在脂质体表面添加聚合涂层可以影响皮肤的输送。递药机制包括完整的囊泡皮肤渗透、游离药物扩散、渗透增强、囊泡吸附到和/或与 SC 融合、跨附件渗透等。最后,一些皮肤状况,包括痤疮、黄褐斑、皮肤老化、真菌感染和皮肤癌,都受益于药物的脂质体局部递送,具有有前途的体外和体内结果。然而,尽管存在一些临床试验,但仍需要进行更多的研究,以探索脂质体在皮肤科领域的潜力。

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