Therapeutic Efficacy of 2‐Methoxyestradiol Microcrystals Encapsulated within Polyelectrolyte Multilayers

Development of a novel formulation of anticancer drugs to improve their water-solubility and bioavailability remains a great challenge. Herein, the potential anticancer agent 2-methoxyestradiol (2-ME) was selected as a model drug and was encapsulated within polyelectrolyte (PE) multilayers by layer-by-layer deposition of oppositely charged PEs onto the drug microcrystal surfaces. Cell viability and morphology observation of two cell lines reveal that the PE multilayer-encapsulated 2-ME microcrystals markedly decrease the cell viability, displaying similar inhibitory effect to that of the conventional formulation of 2-ME dissolved in ethanol. The current approach to encapsulate hydrophobic drug microparticles may be useful for formulating different drugs for a variety of biological applications.