This technical article presents an overview of lipophilic salt forms, which are gaining increasing attention as a way to address formulation and/or biopharmaceutical-related issues, such as poor aqueous solubility, slow dissolution rate, poor chemical stability, and physical stability issues. The design, preparation, and characterization of lipophilic salt forms is described. Preliminary in vitro and in vivo studies also indicate that this salt selection approach is enabling to lipid formulations by supporting substantially higher loadings (>10-fold in some cases) than is otherwise possible using free API.