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Solubilization techniques used for poorly water-soluble drugs

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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.

Poorly water-soluble drugsSolubilization techniquesNanocrystalsCocrystalsIonic liquidsPolymer-based carriersLipid-based carriersInorganic carriers

Bing Xie、Yaping Liu、Xiaotong Li、Pei Yang、Wei He

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School of Pharmacy,China Pharmaceutical University,Nanjing 2111198,China

School of Science,China Pharmaceutical University,Nanjing 2111198,China

Shanghai Skin Disease Hospital,Tongji University School of Medicine,Shanghai 200443,China

2024

药学学报(英文版)

药学学报(英文版)

CSTPCD
ISSN:
年,卷(期):2024.14(11)