title: Advances in P-glycoprotein-based approaches for delivering anticancer drugs: pharmacokinetic perspective and clinical relevance.
abstract: BACKGROUND
  P-glycoprotein (P-gp) is a multi-specific efflux transporter belonging to ATP-binding cassette (ABC) transporter family, encoded by the ABCB1 gene, which significantly impacts the pharmacokinetics as well as multidrug resistance of anticancer drugs.
  
  
  METHODS
  This review explores how human P-gp transporters modulate the pharmacokinetics of anticancer drugs and emerging strategies to modulate their function. The key findings in direct modulation by various P-gp inhibitors on pharmacokinetics of various anticancer P-gp substrates are described. The role of pharmaceutical excipients as P-gp inhibitor with the focus on the recent development in novel drug delivery systems to modulate pharmacokinetics of anticancer drugs is also outlined.
  
  
  CONCLUSIONS
  The concomitant use of anticancer P-gp substrate and P-gp inhibitor is an effective and safe way to enhance the bioavailability of anticancer drugs. The poor bioavailability and toxicity of anticancer drugs limit their therapeutic efficacy. These characteristics can be improved by using various nanocarriers which exhibited a high potential to bypass this efflux protein. The best combination of P-gp inhibitor and substrate anticancer drug in a single nanocarrier formulation is a future challenge and is still probably some years away from the marketplace.
authors.affiliation: Academy of Scientific and Innovative Research (AcSIR), Anusandhan Bhawan , New Delhi-110001 , India.
authors.forename: Ankit
authors.initials: A
authors.lastname: Saneja
authors.forename: Vaibhav
authors.initials: V
authors.lastname: Khare
authors.forename: Noor
authors.initials: N
authors.lastname: Alam
authors.forename: Ravindra Dhar
authors.initials: RD
authors.lastname: Dubey
authors.forename: Prem N
authors.initials: PN
authors.lastname: Gupta
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors / Q000378:metabolism*; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems; D006801:Humans
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000970:Antineoplastic Agents