ABSTRACT
Chemotherapy remains the main treatment for many cancer patients. However, P-glycoprotein (P-gp) mediated multidrug resistance poses severe challenges to current chemotherapies. As ideal vectors to overcome drug resistance, nanovehicles are extensively explored for cancer treatment by diverting P-gp mediated drug efflux mechanisms. Surface engineering of nanocarriers has attracted great attention for targeted therapeutic delivery. The folate receptors, one of the most researched targets in cancer therapeutics, are over-expressed in several carcinomas. And folate has become one of the most investigated ligands in cancer therapeutic direction due to its small size, easy conjugation to nanocarriers, nontoxic, nonimmunogenic nature, and well stability in storage or in circulation. This review discussed the current status of folate functionalized nanoparticles in diverting P-gp mediated drug efflux mechanisms.