Injectable Formulations of Poorly Water-Soluble Drugs
Each year, an increasing number of new molecular entities in the drug development pipeline are characterized as having poor water solubility. While solubility limitations are critically important in all formulations, failure to properly understand and address solubility challenges in parenteral formulations can result in significant toxicities and adverse events. As such, it is imperative that scientists in the parenteral development space understand the vast array of solubilization techniques available for injectable formulations. Relatively simple approaches such as pH manipulation, salt formation, use of a cosolvent system, addition of a surfactant, or complexation may be used to provide sufficient aqueous solubility and favorable drug product properties. More complex approaches may be warranted for tissue targeting, alteration of pharmacokinetic profiles, and sustained drug release.
This chapter provides an overview (though certainly not exhaustive) of applicable formulation approaches, both conventional and investigational, to overcome challenges of poor aqueous solubility. The current authors would like to thank and acknowledge the previous authors’ significant contribution from the first and second editions. This current third edition chapter is a revision and update of the original authors’ work from the first and second editions.
O’Mary, H.L., Cui, Z. (2022). Injectable Formulations of Poorly Water-Soluble Drugs. In: Williams III, R.O., Davis Jr., D.A., Miller, D.A. (eds) Formulating Poorly Water Soluble Drugs. AAPS Advances in the Pharmaceutical Sciences Series, vol 50. Springer, Cham. https://doi.org/10.1007/978-3-030-88719-3_6