Biopharmaceutical study of nanostructured formulation of the anticancer drug derivative of nitrosoalkylurea lysomustine

The aim of this study was to formulate the novel lysomustine (derivative of nitrosoalkylurea) nanostructured dosage form in order to increase the drug bioavailability to tumor cells and reduce its toxicity for normal tissues. In preclinical trials performed on animals, lysomustine has shown significant antineoplastic activity, both in the case of leukemia and solid tumors. On the basis of the results of phase II clinical trials, the Pharmacological committee of the Ministry of Health of the Russian Federation approved the application of lysomustine for treatment of melanoma and lung cancer monotherapy. However, because of its toxicity, the use of this drug in clinical practice has been cancelled. A novel lysomustine nanostructured form has been developed to increase drug bioavailability to tumor cells and reduce damage to normal cells. Investigations have shown that novel lysomustine nanostructured form allows for a widening of the therapeutic range on animals with leucosis (up to 250 mg/kg) without significant toxicity.