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经表面工程改造的治疗药物透过血脑屏障的脂质体递送:最新进展、挑战和机遇。

Surface engineered liposomal delivery of therapeutics across the blood brain barrier: recent advances, challenges and opportunities.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Kalabhavan Campus, The Maharaja Sayajirao University of Baroda, Vadodara, India.

Formulation Development Department-Novel Drug Delivery Systems, Sun Pharmaceutical Industries Ltd, Vadodara, India.

出版信息

Expert Opin Drug Deliv. 2019 Dec;16(12):1287-1311. doi: 10.1080/17425247.2019.1676721.

DOI:10.1080/17425247.2019.1676721
PMID:31581844
Abstract

: The delivery of drug payload to treat various brain diseases are met with various hindrances owing to the presence of the homeostasis regulatory gate, Blood-Brain Barrier (BBB). Although, pathogenesis and progression of the brain diseases alter the permeability of this barrier, effective delivery of agents is not achieved for the attainment of desired treatment outcomes. Liposomes with their salient properties have proven to be exciting options to navigate therapeutics across this barrier.: This review tends to establish a correlation between the pathophysiology of disease affected barrier, with liposome-based passive and active delivery approaches for therapeutic agents, permitting their transport across the BBB. The potential of these carriers to present therapeutically effective agents' concentrations to the desired site of action have also been explored. Further, assessment of physicochemical, biopharmaceutical, and biological properties required for efficient translation of such carriers from bench to bedside has been made.: The encapsulation of the therapeutics in these structures enables suitable pro-brain delivery modifications of inherent pharmacokinetic-pharmacodynamic profiles along with appropriate surface engineering opportunities to deliver the drug cargo to the intended locations in the brain. However, a careful balance between the use of these surface-modified structures and toxicity potential needs to be ascertained for clinical safety and effectiveness.

摘要

: 药物有效载荷的递送用于治疗各种脑部疾病,但由于存在体内平衡调节门(血脑屏障,BBB),因此会遇到各种障碍。尽管脑疾病的发病机制和进展会改变该屏障的通透性,但为了达到预期的治疗效果,无法有效递送药物。具有显著特性的脂质体已被证明是一种很有前途的选择,可以将治疗药物递送到该屏障中:本综述旨在建立疾病影响的屏障的病理生理学与基于脂质体的被动和主动药物传递方法之间的相关性,以允许治疗药物通过血脑屏障。还探讨了这些载体将治疗有效浓度的药物递送到所需作用部位的潜力。此外,还评估了从实验室到临床应用,实现这些载体有效转化所需的物理化学、生物制药和生物学特性:将治疗药物封装在这些结构中,可对固有药代动力学-药效学特性进行适当的亲脑递药修饰,以及进行适当的表面工程,将药物有效负载递送到大脑中的预期部位。然而,为了确保临床安全性和有效性,需要仔细平衡使用这些表面修饰结构和毒性潜力之间的关系。

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