A novel liposomal formulation of FTY720 (Fingolimod) for promising enhanced targeted delivery

We have shown a promising role for FTY720 in treatment of B cell malignancies including chronic and acute lymphocytic leukemias and mantle cell lymphoma. To overcome factors limiting the application of free FTY720 in treating B-cell malignancies, such as relatively low solubility, poor stability in aqueous buffer, and suppression of circulating T lymphocytes, a novel liposomal formulated FTY720 (LP-FTY720) has been developed and characterized. LP-FTY720 exhibited enhanced pharmacokinetics in ICR mice compared to free drug and provided a platform for targeting delivery of FTY720 as well. CD19, CD20 or CD37-targeting based on the LP-FTY720 enhanced the binding efficiency and cytotoxicity compared to non-targeting LP-FTY720 and provided an alternative strategy to achieve potential clinical efficacy in B cell malignancies.92