纳米晶体技术改善中药活性成分成药性的研究进展

Research progress in nanocrystal technology for improving the druggability of active ingredients in traditional Chinese medicine

摘要

许多在药物开发早期阶段具有优良药理效应的中药活性成分,由于水溶性差、膜渗透性低及稳定性不足等成药性问题,其制剂开发与应用受限。纳米晶体技术是将药物颗粒纳米化来改善其制药性能的一种有效策略,能克服中药活性成分的固有缺陷;除作为制剂形式的传统应用途径以外,近年来,该技术还被逐步拓展与Pickering乳液、水凝胶、可溶性微针、微球、脂质体等新型递送系统结合,展现出广阔的应用前景。本文系统梳理了中药活性成分纳米晶的形成机制与理化性质,并从溶解度、溶出度、生物利用度和稳定性4个方面探讨了其改善成药性的潜力和局限性。在此基础上,本文重点综述了纳米晶体融合多种新型递送系统的研究进展,以期为改善中药活性成分的成药性、开发高效制剂提供思路与借鉴。

Abstract

Many active ingredients of traditional Chinese medicine (TCM), exhibiting excellent pharmacological activity in early-stage development, still need to face the formulation development and application challenges due to druggability issues caused by low solubility, poor membrane permeability, and inadequate stability. Nanocrystal technology is an effective strategy that involves nano-sizing drug particles to improve the biopharmaceutics of drug molecules, which can be used to overcome these inherent limitations of TCM active ingredients. Beyond its conventional application as a standalone dosage form, this technology has recently been extended and integrated with novel delivery systems including Pickering emulsions, hydrogels, soluble microneedles, microspheres, and liposomes, demonstrating broad application prospects. This article systematically outlined the formation mechanisms and physicochemical properties of TCM active ingredient nanocrystals, and discussed their capability and constraints in enhancing druggability from four perspectives: solubility, dissolution rate, bioavailability, and stability. Furthermore, we focused on reviewing recent advances in hybrid systems combining nanocrystals with various novel drug delivery platforms, with the aim of offering insights and references to improve the druggability of TCM active ingredients and facilitate the development of efficient formulations.

关键词

中药活性成分 / 纳米晶 / 成药性 / 新型制剂 / 递送系统

Key words

active ingredients in traditional Chinese medicine / nanocrystals / druggability / novel formulations / delivery system

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基金资助

上海市东方英才计划拔尖项目(BJKJ2024041)