A pharmaceutical composition, and methods of use and preparation thereof, beneficial in treating, diagnosing, and preventing a disease, condition, syndrome, or symptoms thereof, characterized by cellular hyperproliferation such as cancer, in warm-blooded animals, including humans, incorporates a lipid nanoemulsion, prepared by processing through homogenization, comprised of lipid particles each comprising at least one non-bilayer- forming lipid capable of being preferentially and selectively actively internalized within a diseased cell an effective amount of at least one therapeutic or diagnostic microtubule- interacting agent associated with the nanoemulsion and a pharmaceutically-acceptable carrier. In a preferred embodiment, the composition may also be comprised of a protein carrier molecule and/or emulsion-enhancing agents such as a surfactant, a plant-based fat source, a solvent, and combinations thereof.
