Development and in vitro evaluation of effervescent floating matrix tablet of neritinib: An anticancer drug

Abstract

Neratinib is a potent anticancer drug, used for the treatment of breast cancer. It is poorly soluble at higher pH, which tends to minimize the therapeutic effects in the lower GIT leads to its poor bioavailability. An attempt has been made to prepare and develop a novel gastro-retentive system of neratinib to improve the drug bioavailability in the GIT by enhancing the gastric retention time. The floating matrix tablets were prepared by various proportions of carbopol 940, micro-crystalline cellulose (MCC) and ethyl cellulose (EC), sodium bicarbonate (NaHCO3) as gas forming agent, by direct compression. The formulation mixture was assessed for pre and post compression test, lag time, in-vitro floating, FTIR, water uptake/swelling index, in vitro and kinetic release studies. The findings revealed that, the parameters of compression (pre and post) were within USP limits. The floating tablets swelled well and floated for more than 24h, with less than 120 seconds of buoyancy lag time. The optimized formulation F3 showed sustained release up to 12h; a non-Fickian mechanism. Therefore, all the results and findings have shown that developed neratinib floating matrix system is a promising approach as a drug delivery system and application in the treatment of breast cancer.