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改善难溶性药物生物利用度的纳米晶体技术:一篇综述

Nanocrystals Technology for Improving Bioavailability of Poorly Soluble Drugs: A Mini-Review.

作者信息

Zhou Yuqi, Du Juan, Wang Lulu, Wang Yancai

出版信息

J Nanosci Nanotechnol. 2017 Jan;17(1):18-28. doi: 10.1166/jnn.2017.13108.

Abstract

Nanocrystals technology for water insoluble drugs delivery has been expanding exponentially, as a robust approach, over the last ten years. Drug nanocrystals are sub-micron colloidal dispersion system of pure drug nanoparticles. Compared to the traditional pharmaceutical dosage forms, nano-crystals formulation presented many extraordinary properties such as enhanced dissolution rate and saturation solubility, high drug loading, excellent reproducibility of oral absorption, improved proportionality of dose-bioavailability, and increased patient compliance. This review explains the bioavailability improving mechanism in drug delivery to present the state-of-art nanocrystals. The physically stable nanocrystals with appropriate particle size and zeta potential could be prepared by screening of stabilizing agents. The marketed nanocrystal products and drug safety issues about the technology are also discussed. Moreover, the perspectives and challenges about improving nanocrystals investigated in this review could provide guidance for further study. Thus, this article could serve as a reference for optimizing the bioavailability of a specific drug candidate.

摘要

在过去十年中,作为一种强大的方法,用于水不溶性药物递送的纳米晶体技术呈指数级增长。药物纳米晶体是纯药物纳米颗粒的亚微米胶体分散体系。与传统药物剂型相比,纳米晶体制剂具有许多非凡的特性,如提高溶解速率和饱和溶解度、高载药量、口服吸收的优异重现性、改善剂量-生物利用度的比例以及提高患者依从性。本综述解释了药物递送中提高生物利用度的机制,以呈现最先进的纳米晶体。通过筛选稳定剂可以制备具有适当粒径和zeta电位的物理稳定纳米晶体。还讨论了市售的纳米晶体产品以及该技术的药物安全性问题。此外,本综述中研究的关于改进纳米晶体的观点和挑战可为进一步研究提供指导。因此,本文可为优化特定候选药物的生物利用度提供参考。

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