The therapeutic efficacy of orally administered drugs is often restricted by their inherent limited oral bioavailability. Low water solubility, limited permeability through the intestinal barrier, instability in harsh environment of the gastrointestinal (GI) tract and being substrate of the efflux pumps and the cytochrome P450 (CYP) can impair oral drug bioavailability resulting in erratic and variable plasma drug profile. As more drugs with low membrane permeability are developed, new interest is growing to enhance their intestinal permeability and bioavailability. A wide variety of nanosystems have been developed to improve drug transport and absorption. Sufficient evidence exists to suggest that nanoparticles are able to increase the transepithelial transport of drug molecules. However, key questions remained unanswered. What types of nanoparticles are more efficient? What are preclinical (or clinical) achievements of each type of nanoformulation in terms of pharmacokinetic (PK) parameters? Addressing this issue in this paper, we have reviewed the current literature regarding permeability enhancement, permeability assessment methods and changes in PK parameters following administration of various nanoformulations. Although permeability enhancement by various nanoformulations holds great promise for oral drug delivery, many challenges still need to be addressed before development of more clinically successful nanoproducts.
Keywords: Intestinal permeability; Marketed nanomedicines; Nanoformulations; Pharmacokinetic properties; Transport mechanisms.
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