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用于中枢神经系统靶向给药的脂质基纳米载体。

Lipid-based nanocarriers for CNS-targeted drug delivery.

作者信息

Micheli Maria-Rita, Bova Rodolfo, Magini Alessandro, Polidoro Mario, Emiliani Carla

机构信息

Department of Experimental Medicine and Biochemical Sciences, University of Perugia, via del Giochetto, 06126 Perugia, Italy.

出版信息

Recent Pat CNS Drug Discov. 2012 Apr 1;7(1):71-86. doi: 10.2174/157488912798842241.

Abstract

Nanotechnology exerts an increasing impact on the development of more effective tools for the diagnosis and treatment of human diseases. This applies in particular to central nervous system (CNS) disorders. Development of therapeutics for CNS is, in fact, one of the most challenging areas in drug development, mainly due to the presence of the blood-brain barrier (BBB) which separates the blood from the cerebral parenchyma thus limiting the brain uptake of the vast majority of neurotherapeutic agents. Among the several strategies which have been developed over the last years in order to overcome this problem, nanotechnology-based approaches have gained increasing attention as the most promising strategies for CNS targeted drug delivery. Nanocarriers offer several advantages such as the possibility to maintain drug levels in a therapeutically desirable range, as well as the increase of half-lives, solubility, stability and permeability of drugs. Furthermore, the system can be designed in such a way as to release the drug in a controlled way or in a triggered way. This review focuses on lipid-based nanocarriers and more specifically on liposomes, lipid-core micelles, and lipid nanocapsules, and provides an update on their composition and use, including recent patents in the field.

摘要

纳米技术对开发更有效的人类疾病诊断和治疗工具的影响日益增大。这尤其适用于中枢神经系统(CNS)疾病。事实上,中枢神经系统治疗药物的开发是药物开发中最具挑战性的领域之一,主要是因为存在血脑屏障(BBB),它将血液与脑实质分隔开,从而限制了绝大多数神经治疗药物进入大脑。在过去几年中为克服这一问题而开发的几种策略中,基于纳米技术的方法作为中枢神经系统靶向给药最有前景的策略受到越来越多的关注。纳米载体具有多种优势,例如能够将药物水平维持在治疗所需范围内,以及延长药物的半衰期、提高溶解度、稳定性和渗透性。此外,该系统可以设计成以可控方式或触发方式释放药物。本综述聚焦于基于脂质的纳米载体,更具体地说是脂质体、脂质核胶束和脂质纳米囊,并提供了它们的组成和应用的最新信息,包括该领域的近期专利。

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