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脂质体纳米药物。

Liposomal nanomedicines.

作者信息

Fenske David B, Cullis Pieter R

机构信息

Department of Chemistry, University College of the Fraser Valley, 33844 King Road, Abbotsford, BC, V2S 7M8, Canada.

出版信息

Expert Opin Drug Deliv. 2008 Jan;5(1):25-44. doi: 10.1517/17425247.5.1.25.

Abstract

Liposomal nanoparticles (LNs) encapsulating therapeutic agents, or liposomal nanomedicines, represent an advanced class of drug delivery systems, with several formulations presently on the market and many more in clinical trials. Over the past 20 years, a variety of techniques have been developed for encapsulating both conventional drugs (such as anticancer drugs and antibiotics) and the new genetic drugs (plasmid DNA containing therapeutic genes, antisense oligonucleotides and small interfering RNA) within LNs. If the LNs possess certain properties, they tend to accumulate at sites of disease, such as tumours, where the endothelial layer is 'leaky' and allows extravasation of particles with small diameters. These properties include a diameter centred on 100 nm, a high drug-to-lipid ratio, excellent retention of the encapsulated drug, and a long (> 6 h) circulation lifetime. These properties permit the LNs to protect their contents during circulation, prevent contact with healthy tissues, and accumulate at sites of disease. The authors discuss recent advances in this field involving conventional anticancer drugs, as well as applications involving gene delivery, stimulation of the immune system and silencing of unwanted gene expression. Liposomal nanomedicines have the potential to offer new treatments in such areas as cancer therapy, vaccine development and cholesterol management.

摘要

包裹治疗剂的脂质体纳米颗粒(LNs),即脂质体纳米药物,是一类先进的药物递送系统,目前有多种制剂已上市,还有更多正在进行临床试验。在过去20年里,已开发出多种技术用于将传统药物(如抗癌药物和抗生素)以及新型基因药物(含有治疗基因的质粒DNA、反义寡核苷酸和小干扰RNA)包裹在脂质体纳米颗粒中。如果脂质体纳米颗粒具有某些特性,它们往往会在疾病部位(如肿瘤)积聚,肿瘤部位的内皮细胞层“有渗漏”,允许小直径颗粒外渗。这些特性包括直径以100纳米为中心、高药物与脂质比、对包裹药物的良好保留以及长(>6小时)循环寿命。这些特性使脂质体纳米颗粒在循环过程中能够保护其内容物,防止与健康组织接触,并在疾病部位积聚。作者讨论了该领域涉及传统抗癌药物的最新进展,以及涉及基因递送、免疫系统刺激和有害基因表达沉默的应用。脂质体纳米药物有潜力在癌症治疗、疫苗开发和胆固醇管理等领域提供新的治疗方法。

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