Analysis and optimization of drug solubility to improve pharmacokinetics

Abstract

Solubility measurement is one of the key elements that need to be considered in drug discovery and development process. Hence, its appropriate analysis and optimization is necessary to enhance the drug’s pharmacokinetic and therapeutic effects. In this article, different methods used for solubility analysis and optimization such as shake flask, potentiometric, turbidimetric, computational, miniature device and high throughput automated methods have been summarized. Additionally, the effect of solubility optimization methods (physical, chemical and carrier technology modifications) on pharmacokinetic enhancement has also been elucidated. New fast, feasible and automated methods of solubility analysis are necessary for its accurate measurement as well as for minimization of errors posed by traditional methods. Among the physical, chemical and carrier modification methods; higher potential is exhibited by nanoparticulate drug delivery carriers for optimization of drug solubility and enhancement of pharmacokinetics. Based on the drug characteristics and delivery requirement, appropriate method can be chosen for efficient solubility and pharmacokinetics enhancement of lipophilic drugs, especially of BCS class II and class IV.