Advanced screening assays to rapidly identify solubility-enhancing formulations: high-throughput, miniaturization and automation.
Development of solubility-enhancing formulations for poorly water-soluble compounds always poses a challenge. Conventional formulation screening assays are potentially time-consuming and labor-intensive and, moreover, require a large amount of a compound; they are not ideal when compound availability and testing time are limited. In recent years, in-vitro screening assays that are rapid, inexpensive, minimally labor-intensive, and require only small quantities of a compound have become available. These advanced assays allow high-throughput automation, miniaturization, and parallel processing, thereby enabling scientists to rapidly identify solubility-enhancing formulations with milligram or sub-milligram quantities of an active pharmaceutical ingredient (API). This article reviews these assays for rapidly screening the aqueous solubility of lead compounds and the solubility-enhancing formulations with limited quantities of API.
Dai
Wei-Guo
WG
Pharmaceutical Development, ALZA Corporation, 1900 Charleston Road, Mountain View, CA 94039, USA. wdai2@alzus.jnj.com
Pollock-Dove
Crystal
C
Dong
Liang C
LC
Li
Shu
S
D001331:Automation / Q000379:methods; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D007700:Kinetics; D008904:Miniaturization / Q000379:methods*; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D012995:Solubility; D012997:Solvents; D013816:Thermodynamics
D004364:Pharmaceutical Preparations; D012997:Solvents