中国中药杂志2025，Vol.50Issue(16)：4471-4482,12.DOI:10.19540/j.cnki.cjcmm.20250321.303
基于聚合物过饱和自纳米乳递药技术的难溶性药物口服制剂开发
Development of oral preparations of poorly soluble drugs based on polymer supersaturated self-nanoemulsifying drug delivery technology
摘要
Abstract
Poor water solubility is the primary obstacle preventing the development of many pharmacologically active compounds into oral preparations.Self-nanoemulsifying drug delivery systems(SNEDDS)have become a widely used strategy to enhance the oral bioavailability of poorly soluble drugs by inducing a supersaturated state,thereby improving their apparent solubility and dissolution rate.However,the supersaturated solutions formed in SNEDDS are thermodynamically unstable systems with solubility levels exceeding the crystalline equilibrium solubility,making them prone to drug precipitation in the gastrointestinal tract and ultimately hindering drug absorption.Therefore,maintaining a stable supersaturated state is crucial for the effective delivery of poorly soluble drugs.Incorporating polymers as precipitation inhibitors(PPIs)into the formulation of supersaturated self-nanoemulsifying drug delivery systems(S-SNEDDS)can inhibit drug aggregation and crystallization,thus maintaining a stable supersaturated state.This has emerged as a novel preparation strategy and a key focus in SNEDDS research.This review explores the preparation design of SNEDDS and the technical challenges involved,with a particular focus on polymer-based S-SNEDDS for enhancing the solubility and oral bioavailability of poorly soluble drugs.It further elucidates the mechanisms by which polymers participate in transmembrane transport,summarizes the principles by which polymers sustain a supersaturated state,and discusses strategies for enhancing drug absorption.Altogether,this review provides a structured framework for the development of S-SNEDDS preparations with stable quality and reduced development risk,and offers a theoretical reference for the application of S-SNEDDS technology in improving the oral bioavailability of poorly soluble drugs.关键词
聚合物过饱和自纳米乳/稳定性/难溶性药物/口服药物递送系统开发Key words
polymer supersaturated self-nanoemulsion/stability/poorly soluble drug/development of oral drug delivery system引用本文复制引用
陈绪龙,李成,沈姜雯,查炜玮,易建云,李林,赖章婷,廖正根,朱烨,程悦尔..基于聚合物过饱和自纳米乳递药技术的难溶性药物口服制剂开发[J].中国中药杂志,2025,50(16):4471-4482,12.基金项目
江西省自然科学基金面上项目(20242BAB25578) （20242BAB25578）
江西省卫生健康委员会项目(202212007) （202212007）
江西省中医药管理局项目(2022A137,2023B1287) （2022A137,2023B1287）
北京医学健康基金会项目(TYU046B) （TYU046B）
北京医学奖励基金会项目(YXJL-2022-0734-0294) （YXJL-2022-0734-0294）
北京健康联盟慈善基金会项目(B22010) （B22010）
