RT Journal Article ID 198950564440242d A1 Mittal, Karan A1 Patadia, Riddhish A1 Vora, Chintan A1 Mashru, Rajashree T1 Myriad Molecules to Overcome Efflux Drug Transporters and Drug-Metabolizing Enzymes: A Journey from Synthetic to Natural JF Critical Reviews™ in Therapeutic Drug Carrier Systems JO CRT YR 2015 FD 2015-06-29 VO 32 IS 5 SP 441 OP 460 K1 bioenhancer K1 biopharmaceutics drug disposition classification system K1 CYP enzyme K1 excipients K1 novel drug-delivery system K1 P-gp AB 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. PB Begell House LK https://www.dl.begellhouse.com/journals/3667c4ae6e8fd136,79fe062853567e52,198950564440242d.html