Evaluating dasatinib nanocarrier: Physicochemical properties and cytotoxicity activity on cancer cells.

Abstract

Objective: Dasatinib-(DAS) is a tyrosine kinase inhibitor usually used to treat leukemia. However, DAS is a poorly water-soluble drug. Therefore, oil-in-water emulsions were used for DAS to enhance its solubility and cancer treatment efficacy. This study aims to develop an appropriate DAS nanoemulsion (NE) that can overcome the issue of DAS solubility and provide an effective anticancer effect.

Methods: Spherical particles dispersed in an aqueous media approach within an oily phase (oleic acid, Kolliphor RH40, and dipropylene glycol) were used to formulate DAS-NE using high-energy methods. Different formulas were developed and an appropriate formula was analyzed to identify its physicochemical properties. Raw DAS and nonformula cytotoxicity were evaluated through MTT assay against three cancer cell lines, MCF7 (human breast adenocarcinoma), HT29, and SW480 (human colorectal carcinomas), in addition to MRC5 (Normal human fetal lung fibroblast).

Results: Different DAS-NEs (1-7) have been developed successfully. Formulas had a droplet size of a diameter ranging from 84.167 ± 10.178 nm to 273.433 ± 45.267 nm. The drug content of the appropriate formula (DAS-NE₃) was found to be 83.2%. The drug release result of DAS-NE₃ when compared to raw DAS was about 58%, falling to 13% after 24 h. The DAS-NE₃ showed cytotoxicity against the three cancer cells below 26.11 μM but showed 30-fold significantly increased selectivity against MRC5 normal cells compared to that of raw DAS.

Conclusion: This study shows that the DAS-NE₃ formula may provide a potentially effective and sustained drug delivery for cancer treatment. This provides valuable information to the scientific community and the pharmaceutical industry.