We develop methods for modifying basic physicochemical properties of drugs so as to assign desired characteristics to the final dosage form. We design readily bioavailable nanometric drug delivery systems with improved biodistribution properties for various delivery routes. We focus on addressing widespread challenges associated with nanoparticle synthesis, e.g., uncontrollable crystallization and crystal growth, particle aggregation and size increase, loss of API activity, insufficient carrier biocompatibility/biodegradability and more.We develop methods for modifying basic physicochemical properties of drugs so as to assign desired characteristics to the final dosage form. We design readily bioavailable nanometric drug delivery systems with improved biodistribution properties for various delivery routes. We focus on addressing widespread challenges associated with nanoparticle synthesis, e.g., uncontrollable crystallization and crystal growth, particle aggregation and size increase, loss of API activity, insufficient carrier biocompatibility/biodegradability and more.