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纳米载体及其改善皮肤渗透性和经皮给药的作用。

Nanocarriers and their Actions to Improve Skin Permeability and Transdermal Drug Delivery.

作者信息

Khan Nauman R, Harun Mohd S, Nawaz Asif, Harjoh Nurulaini, Wong Tin W

机构信息

Non-Destructive Biomedical and Pharmaceutical Research Centre, Universiti Teknologi MARA, Puncak Alam, 42300, Selangor, Malaysia.

出版信息

Curr Pharm Des. 2015;21(20):2848-66. doi: 10.2174/1381612821666150428145216.

DOI:10.2174/1381612821666150428145216
PMID:25925113
Abstract

Transdermal drug delivery is impeded by the natural barrier of epidermis namely stratum corneum. This limits the route to transport of drugs with a log octanol-water partition coefficient of 1 to 3, molecular weight of less than 500 Da and melting point of less than 200°C. Nanotechnology has received widespread investigation as nanocarriers are deemed to be able to fluidize the stratum corneum as a function of size, shape, surface charges, and hydrophilicity-hydrophobicity balance, while delivering drugs across the skin barrier. This review provides an overview and update on the latest designs of liposomes, ethosomes, transfersomes, niosomes, magnetosomes, oilin- water nanoemulsions, water-in-oil nanoemulsions, bicontinuous nanoemulsions, covalently crosslinked polysaccharide nanoparticles, ionically crosslinked polysaccharide nanoparticles, polyelectrolyte coacervated nanoparticles and hydrophobically modified polysaccharide nanoparticles with respect to their ability to fuse or fluidize lipid/protein/tight junction regimes of skin, and effect changes in skin permeability and drug flux. Universal relationships of nanocarrier size, zeta potential and chemical composition on transdermal permeation characteristics of drugs will be developed and discussed.

摘要

经皮给药受到表皮天然屏障即角质层的阻碍。这限制了具有1至3的正辛醇 - 水分配系数、小于500道尔顿的分子量和小于200°C熔点的药物的转运途径。由于纳米载体被认为能够根据尺寸、形状、表面电荷和亲水 - 疏水平衡使角质层流化,同时将药物输送穿过皮肤屏障,因此纳米技术受到了广泛研究。本综述概述并更新了脂质体、醇质体、传递体、非离子脂质体、磁小体、水包油纳米乳液、油包水纳米乳液、双连续纳米乳液、共价交联多糖纳米颗粒、离子交联多糖纳米颗粒、聚电解质凝聚纳米颗粒和疏水改性多糖纳米颗粒的最新设计,涉及它们融合或流化皮肤脂质/蛋白质/紧密连接区域的能力,以及对皮肤渗透性和药物通量的影响变化。将开发并讨论纳米载体尺寸、zeta电位和化学成分与药物经皮渗透特性之间的普遍关系。

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