Solubilization techniques used for poorly water-soluble drugs  

作　　者：Bing Xie Yaping Liu Xiaotong Li Pei Yang Wei He 

机构地区：[1]School of Pharmacy,China Pharmaceutical University,Nanjing 2111198,China [2]School of Science,China Pharmaceutical University,Nanjing 2111198,China [3]Shanghai Skin Disease Hospital,Tongji University School of Medicine,Shanghai 200443,China

出　　处：《Acta Pharmaceutica Sinica B》2024年第11期4683-4716,共34页药学学报（英文版）

基　　金：National Natural Science Foundation of China(Nos.82073782 and 82241002).

摘　　要：About 40%of approved drugs and nearly 90%of drug candidates are poorly water-soluble drugs.Low solubility reduces the drugability.Effectively improving the solubility and bioavailability of poorly water-soluble drugs is a critical issue that needs to be urgently addressed in drug development and application.This review briefly introduces the conventional solubilization techniques such as solubili-zers,hydrotropes,cosolvents,prodrugs,salt modification,micronization,cyclodextrin inclusion,solid dispersions,and details the crystallization strategies,ionic liquids,and polymer-based,lipid-based,and inorganic-based carriers in improving solubility and bioavailability.Some of the most commonly used approved carrier materials for solubilization techniques are presented.Several approved poorly water-soluble drugs using solubilization techniques are summarized.Furthermore,this review summa-rizes the solubilization mechanism of each solubilization technique,reviews the latest research advances and challenges,and evaluates the potential for clinical translation.This review could guide the selection of a solubilization approach,dosage form,and administration route for poorly water-soluble drugs.Moreover,we discuss several promising solubilization techniques attracting increasing attention worldwide.

关 键 词：Poorly water-soluble drugs Solubilization techniques Nanocrystals COCRYSTALS Ionic liquids Polymer-based carriers Lipid-based carriers Inorganiccarriers 

分 类 号：R91[医药卫生—药学]