Background: P-glycoprotein (P-gp), a well known ATP dependent efflux membrane
transporter, has been attracting considerable interests of medical researchers due to its efflux
pump effect being a primary cause of multidrug resistance (MDR) and poor bioavailability (BA)
of anticancer agents. How to resolve the aforesaid problems has become the research hot-points
in the medical and pharmaceutical fields. The past three decades have witnessed rapid development
of the P-gp inhibition-based strategies used for modulating pharmacokinetics (PK) and thus
overcoming MDR and improving BA of anticancer drugs.
Methods: An electronic search of PubMed database from inception to April, 2016 was conducted.
Additionally, we searched the reference lists of included studies and carried out a citation
search for the included studies via Web of Science to find other potentially relevant studies.
Results and Conclusion: Lots of the studies of the P-gp inhibition-based strategies are under
preclinical phase and the obtained results are exciting and may represent great promise in the
clinical application potential. In order to provide useful information for the development of novel strategies for improving
BA of anticancer drugs, this article aims to review the research progress in the P-gp inhibition-based strategies
that has been acquired over the last three decades, with focus on the P-gp inhibitors, herbal constituents and pharmaceutical
excipients as well as novel P-gp-linked drug delivery systems (DDSs). Additionally, the fundamental knowledge
on P-gp also is briefly discussed.