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纳米载体:提高天然成分溶解度、稳定性和优化生物功效的有效工具。

Nanocarriers: A Successful Tool to Increase Solubility, Stability and Optimise Bioefficacy of Natural Constituents.

机构信息

Department of Chemistry "Ugo Schiff", University of Florence, via Ugo Schiff 6, 50121, Sesto Fiorentino, Florence, Italy.

Institute of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Yuquan Road 88, Tianjin, 300193, China.

出版信息

Curr Med Chem. 2019;26(24):4631-4656. doi: 10.2174/0929867325666181101110050.

Abstract

Natural products are fascinating molecules in drug discovery for their exciting structure variability and also for their interaction with various targets. Drugs multi-targeting effect represents a more realistic approach to develop successful medications for many diseases. However, besides a large number of successful in vitro and in vivo studies, most of the clinical trials fail. This is generally related to the scarce water solubility, low lipophilicity and inappropriate molecular size of natural compounds, which undergo structural instability in biological milieu, rapid clearance and high metabolic rate. Additionally, some molecules are destroyed in gastric juice or suffer to a massive pre-systemic metabolism in the liver, when administered orally, limiting their clinical use. A reduced bioavailability can also be linked to drug distribution/accumulation in non-targeted tissues and organs that increase the side effects lowering the therapeutic efficacy and patient compliance. Nanomedicine represents a favourable tool to increase bioavailability and activities of natural products. Generally, nanovectors provide a large surface area and can overcome anatomic barriers. Each nanovector has its own advantages, disadvantages, and characteristics. In this review, different nanocarriers made of compounds which are Generally Recognized As Safe (GRAS) for the delivery of natural products, marketed as food supplements and medicines are reported.

摘要

天然产物是药物发现中引人入胜的分子,其结构多变性以及与各种靶点的相互作用使其成为药物研发的热点。药物多靶效应代表了一种更现实的方法,可以开发出许多疾病的成功药物。然而,除了大量的体外和体内研究成功之外,大多数临床试验都失败了。这通常与天然化合物的水溶性差、脂溶性低和分子大小不合适有关,这些化合物在生物环境中结构不稳定,清除速度快,代谢率高。此外,一些分子在口服给药时会在胃液中被破坏,或者在肝脏中受到大量的预系统性代谢,从而限制了它们的临床应用。生物利用度降低也可能与药物在非靶向组织和器官中的分布/积累有关,这会增加副作用,降低治疗效果和患者依从性。纳米医学是提高天然产物生物利用度和活性的一种有利工具。一般来说,纳米载体提供了更大的表面积,可以克服解剖屏障。每种纳米载体都有其自身的优点、缺点和特性。在这篇综述中,报道了不同的由一般认为安全(GRAS)化合物制成的纳米载体,用于天然产物的输送,这些化合物被作为食品补充剂和药物销售。

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