Evaluation of the effects of a dasatinib-containing, self-emulsifying, drug delivery system on HT29 and SW420 human colorectal carcinoma cells, and MCF7 human breast adenocarcinoma cells.

BACKGROUND/AIM: Dasatinib (DS), a second-generation tyrosine kinase inhibitor, functions as a multi-target small-molecule drug via targeting various tyrosine kinases involved in neoplastic cell growth. DS inhibits cancer cell replication and migration, and induces tumor cell apoptosis in a variety of solid tumors. However, it is poorly soluble in water under some pH values. Therefore, the development of a DS-containing, self-emulsifying, drug delivery system (SeDDs) could help overcome these problems in treating cancer cells.

METHODS

Various SeDD formulations loaded with DS were developed with isopropyl myristate (oil phase), Labrafil (surfactant), and polyethylene glycol (co-surfactant). The physicochemical properties of the formulations were assessed according to droplet size, encapsulation efficiency, and in vitro drug release. The cytotoxicity of the formulations on the cancer cell lines HT29 and SW420 (human colorectal carcinoma), and MCF7 (human breast adenocarcinoma), in addition to MRC5 normal human fetal lung fibroblasts, was evaluated to assess selectivity.

RESULTS

The DS-SeDD formulation showed favorable particle size, encapsulation efficiency, and in vitro drug release. The anti-cancer potency of DS-SeDDs had greater cytotoxicity effects than pure DA on the three cancer cell lines, MCF7, HT29, and SW420l.

CONCLUSION

The developed DS-SeDD formulations may potentially be an effective sustained drug delivery method for cancer therapy.