Solubilization techniques used for poorly water-soluble drugs.
10.1016/j.apsb.2024.08.027
- Author:
Bing XIE
1
;
Yaping LIU
1
;
Xiaotong LI
1
;
Pei YANG
2
;
Wei HE
3
Author Information
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.
- Publication Type:Review
- Keywords:
Cocrystals;
Inorganic carriers;
Ionic liquids;
Lipid-based carriers;
Nanocrystals;
Polymer-based carriers;
Poorly water-soluble drugs;
Solubilization techniques
- From:
Acta Pharmaceutica Sinica B
2024;14(11):4683-4716
- CountryChina
- Language:English
-
Abstract:
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 solubilizers, 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 summarizes 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.
