In vivo evaluation of a self-nanoemulsifying drug delivery system for sunitinib

Introduction: 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 a multi-targeted receptor tyrosine kinase inhibitor that inhibits tumor cell proliferation and angiogenesis, and has been administrated as an anticancer drug. Self-nanoemulsifying drug delivery system (SNEDDS) is an isotopic mixture of an oil, a surfactant and usually a co-surfactant, which can spontaneously form fine oil-in-water nanoemulsion in aqueous media. Methods: In this study, a SNEDDS composed of ۱۵% ethyl oleate, ۳۰% tween ۸۰, and ۵۵% PEG ۶۰۰ was prepared and developed as a carrier for sunitinib. To inspect the bioavailability of the drug-loaded SNEDDS after oral administration with a dose of ۵۰ mg kg−۱, the maximum plasma concentration and the mean area under the plasma concentration-time curve were measured. Results: The results showed that Cmax and AUC of sunitinib increased respectively by ۱.۴۵ and ۱.۲۴ times using SNEDDS, compared to the suspension implying the effectiveness of SNEDDS for improving the oral bioavailability of sunitinib. In addition, Tmax was shorter for the SNEDDS indicating increasing in the solubility and more rapid absorption of the drug by the nanoemulsion formation. Conclusion: SNEDDS provides an opportunity for the improvement of performance of drugs with poor water solubility and thus serves as an ideal carrier for the delivery of such drugs. In the present study, sunitinib-SNEDDS was prepared, and evaluated in vivo. Our results indicated that oral sunitinib administration was also improved upon loading in SNEDDS.

کلیدواژه ها:

Sutent ، Bioavailability ، Emulsion ، Drug delivery