An Overview on Tyrosine Kinase Inhibitor Gefitinib Drug Delivery Systems for Enhanced Treatment of Cancer

ABSTRACT: IRESSA (gefitinib), an oral drug used once daily at a dose of 250 mg, suppresses the activity of the epidermal growth factor receptor tyrosine kinase (EGFR-TK). Having been granted a license for the first EGFR-TK inhibitor to treat non-small cell lung cancer, it is presently acknowledged in over 70 countries worldwide. Extensive research has been devoted to examining its beneficial impacts on human health, encompassing anti-oxidant, anti-inflammatory, cardioprotective, and anti-tumor properties. The development of therapeutic applications is hampered by the low bioavailability (BA) of gefitinib, which appears to be a severe limitation on the drug's in vivo biological effects. Within this particular framework, a growing sum of current research has focused on developing innovative gefitinib formulations to get beyond their low solubility, restricted stability, excessive metabolization, and inadequate BA. This study addresses the physicochemical and pharmacokinetic (PK) constraints on gefitinib BA, discusses the preparations that have been tried for the administration, controlled release, and targeting of gefitinib, and pinpoints potential forthcoming routes for gefitinib delivery.