A novel self-nanoemulsifying formulation for sunitinib: evaluation of anticancer efficacy

Introduction & Aim: Breast cancer is the top cancer and a main cause of death among women. The incidence of this cancer is increasing in the world. Sunitinib maleate is an oral, small-molecule, multi-targeted receptor tyrosine kinase inhibitor that inhibits tumor cell growth and angiogenesis. However, its efficacy has been limited due to its side effects, and this limitation can be overcome by novel drug delivery systems. Self-nanoemulsifying drug delivery system (SNEDDS) is an isotopic mixture which can spontaneously form fine oil-in-water nanoemulsion in aqueous media. Methods: In the present study, a SNEDDS comprising ethyl oleate, tween 80 and polyethylene glycol (PEG) 600 for sunitinib was design, characterized, and evaluated in vivo.Results: A SNEDDS formulation consists of 15% ethyloleate (as an oil phase), 30% tween 80 (as a surfactant), and 55% PEG 600 (as a co-surfactant) was developed as a carrier for sunitinib. The average particle size of sunitinib loaded SNEDDS was 29.56.3 nm. Sunitinib released from SNEDDS was increased accompanied by a controlled dissolution of the drug. Cytotoxicity studies on 4T1 and MCF-7 cell lines revealed a toxicity enhancement in sunitinib by SNEDDS. To inspect the bioavailability of the drug loaded SNEDDS after oral administration with a dose of 50 mg kg-1,the maximum plasma concentration and the mean area under the plasma concentration-time curve were calculated. It was found that these parameters were increased 1.45- and 1.24-times respectively, compared to a drug suspension.Conclusion: SNEDDS providesan opportunity for the improvement of performance of new drugs.

کلیدواژه ها:

Sutent ، Bioavailability ، Emulsion ، Drug delivery