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基于体内理化参数的生物医学树枝状聚合物空间探索:关键因素分析(第 2 部分)。

Exploration of biomedical dendrimer space based on in-vivo physicochemical parameters: Key factor analysis (Part 2).

机构信息

Université Paris Descartes, PRES Sorbonne Paris Cité, CNRS UMR 860, Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologique, 45, rue des Saints Peres, 75006 Paris, France; CQM - Centro de Química da Madeira, MMRG, Universidade da Madeira, Campus da Penteada, 9020-105 Funchal, Portugal; Glycovax Pharma, 424 Guy Street, Suite 202, Montreal, Quebec H3J 1S6, Canada; Department of Pharmacy, Zhengzhou Railway Vocational & Technical College, Zhengzhou 450018, China.

CQM - Centro de Química da Madeira, MMRG, Universidade da Madeira, Campus da Penteada, 9020-105 Funchal, Portugal; School of Materials Science and Engineering/Center for Nano Energy Materials, Northwestern Polytechnical University, Xi'an 710072, China.

出版信息

Drug Discov Today. 2019 May;24(5):1184-1192. doi: 10.1016/j.drudis.2019.03.001. Epub 2019 Mar 21.

DOI:10.1016/j.drudis.2019.03.001
PMID:30904723
Abstract

In nanomedicine, the widespread concern of nanoparticles in general, and dendrimers, in particular, is the analysis of key in-vivo physicochemical parameters to ensure the preclinical and clinical development of 'safe' bioactive nanomaterials. It is clear that for biomedical applications, biocompatible dendrimers, used as nanocarriers or active per se, should be devoid of toxicity and immunogenicity, and have adequate PK/PD behaviors (adequate exposure) in order to diffuse in different tissues. Functionalization of dendrimers has a dramatic effect on in-vivo physicochemical parameters. In this review, we highlighted key in-vivo physicochemical properties, based on data from biochemical, cellular and animal models, to provide biocompatible dendrimers. Up-to-date, only scarce studies have been described on this topic.

摘要

在纳米医学中,普遍关注纳米颗粒,尤其是树状大分子,是分析关键的体内理化参数,以确保“安全”生物活性纳米材料的临床前和临床开发。显然,对于生物医学应用,作为纳米载体或本身具有活性的生物相容树状大分子,应该没有毒性和免疫原性,并具有适当的 PK/PD 行为(足够的暴露),以便在不同组织中扩散。树状大分子的功能化对体内理化参数有显著影响。在这篇综述中,我们根据来自生化、细胞和动物模型的数据,强调了关键的体内理化特性,以提供生物相容的树状大分子。迄今为止,关于这个主题的描述只有少数。

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