title: Myriad Molecules to Overcome Efflux Drug Transporters and Drug-Metabolizing Enzymes: A Journey from Synthetic to Natural.
abstract: A vast range of prescribed drugs suffers from low and variable bioavailability mainly because of metabolism and permeation complications. This issue of bioavailability is a key problem that has been ongoing for many years. Various tactics have been introduced that have been quite beneficial for improving the bioavailability of poorly bioavailable drugs. Some of these tactics are targeted on cytochrome-P450 (CYP) enzymes and the permeability-glycoprotein (P-gp) efflux pump. Strategies include small-molecule inhibitors, novel drug-delivery systems, pharmaceutical synthetic excipients, and natural bioenhancers. This review discusses the role of synthetic excipients and natural bioenhancers in potentiating the activity of poorly bioavailable drugs, including their pharmacological background and their future applicability to health care. The molecules of synthetic origin such as Gelucire and those of natural origin such as quercetin and silibinin can provide noteworthy benefits to patients and the health care system by helping to reduce dosing and drug side effects.
authors.affiliation: Pharmacy Department, Faculty of Technology and Engineering, The Maharaja Sayajirao University of Baroda, Kalabhavan, Vadodara-390001, Gujarat State, India.
authors.forename: Karan
authors.initials: K
authors.lastname: Mittal
authors.affiliation: Pharmacy Department, Faculty of Technology and Engineering, The Maharaja Sayajirao University of Baroda, Kalabhavan, Vadodara-390001, Gujarat State, India.
authors.forename: Riddhish
authors.initials: R
authors.lastname: Patadia
authors.affiliation: Pharmacy Department, Faculty of Technology and Engineering, The Maharaja Sayajirao University of Baroda, Kalabhavan, Vadodara-390001, Gujarat State, India.
authors.forename: Chintan
authors.initials: C
authors.lastname: Vora
authors.affiliation: Pharmacy Department, Faculty of Technology and Engineering, The Maharaja Sayajirao University of Baroda, Kalabhavan, Vadodara-390001, Gujarat State, India.
authors.forename: Rajashree
authors.initials: R
authors.lastname: Mashru
mesh_terms: D000818:Animals; D001682:Biological Availability; D065607:Cytochrome P-450 Enzyme Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D016503:Drug Delivery Systems; D005079:Excipients / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D026901:Membrane Transport Proteins / Q000187:drug effects* / Q000378:metabolism*; D010599:Pharmacokinetics
chemical_list: D065607:Cytochrome P-450 Enzyme Inhibitors; D005079:Excipients; D026901:Membrane Transport Proteins