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脂质体在药物传递中的应用:专利审查(2007 年至今)。

Liposomes in drug delivery: a patent review (2007 - present).

机构信息

University of Granada, Faculty of Pharmacy, Department of Pharmacy and Pharmaceutical Technology , Campus Universitario de Cartuja s/n, 18071 Granada , Spain +34 958 24 39 02 ; +34 958 24 89 58 ;

出版信息

Expert Opin Ther Pat. 2013 Nov;23(11):1399-414. doi: 10.1517/13543776.2013.828035. Epub 2013 Aug 19.

Abstract

INTRODUCTION

Drug therapy is frequently limited by the widespread biodistribution of the active agents and the little specificity for non-healthy cells. Therefore, inadequate drug concentrations result into the site of action, and severe toxicity may also arise. To address the problem, liposome-based medicines have tried to improve pharmacotherapy.

AREAS COVERED

The review provides an updated revision of the lately published patents covering recent advances in liposome-based drug delivery. They are principally related to the control of drug biodistribution by using stealth, stimuli-sensitive and/or liposomal structures surface modified for ligand-mediated delivery. The contribution further highlights liposome-based theranosis.

EXPERT OPINION

Liposomes have received great attention given their biocompatibility, biodegradability and targetability. From 2007 to present date, patent publications related to their use in drug delivery have shown the move towards more stable structures with optimized drug delivery capabilities, further combining passive and active targeting concepts to gain control of the in vivo fate. However, the introduction of all these liposomal structures in the disease arena is still a challenge. Two key aspects are the difficulty of identifying easy and economic synthesis conditions which can be scaled up in the pharmaceutical industry, and the need for complementary investigations illustrating risks of toxicity/immunogenicity.

摘要

简介

药物治疗常常受到活性药物广泛的生物分布和对非健康细胞的低特异性的限制。因此,作用部位的药物浓度不足,也可能会产生严重的毒性。为了解决这个问题,基于脂质体的药物已经尝试改善药物治疗。

涵盖领域

该综述提供了对最近发表的专利的最新修订,这些专利涵盖了基于脂质体的药物输送的最新进展。它们主要与通过使用隐形、刺激敏感和/或用于配体介导输送的脂质体结构表面修饰来控制药物的生物分布有关。该综述进一步强调了基于脂质体的治疗。

专家意见

由于脂质体具有生物相容性、生物降解性和靶向性,因此受到了广泛关注。从 2007 年至今,与脂质体在药物输送中的应用相关的专利出版物表明,人们越来越关注具有优化药物输送能力的更稳定结构,进一步将被动和主动靶向概念结合起来,以控制体内命运。然而,将所有这些脂质体结构引入疾病领域仍然是一个挑战。两个关键方面是确定易于和经济的合成条件的困难,这些条件可以在制药行业中扩大规模,以及需要补充说明毒性/免疫原性风险的研究。

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