title: Nanocarriers protecting toward an intestinal pre-uptake metabolism.
abstract: Pre-uptake metabolism within the GI tract is responsible for the poor oral bioavailability of numerous drugs. As nanocarriers function as a 'shield', protecting incorporated drugs from enzymatic attack, there is an increasing interest in utilizing them as a tool for overcoming drug degradation. Degradation of carriers resulting in the release of incorporated drugs, mucus permeation, enzyme inhibitory properties and their toxicity are crucial factors that must be taken into account when designing proper nanocarriers. The use of polymer- and lipid-based nanocarriers as protective vehicles are discussed within this review. Lipid-based carriers and novel mucopenetrating particles seem to have a great potential in avoiding metabolizing enzymes. Accordingly, nanocarriers are promising tools for improving the bioavailability of drugs, being sensitive to a pre-uptake metabolism.
authors.affiliation: Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, A-6020 Innsbruck, Austria.
authors.forename: Wongsakorn
authors.initials: W
authors.lastname: Suchaoin
authors.affiliation: Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, A-6020 Innsbruck, Austria.
authors.forename: Andreas
authors.initials: A
authors.lastname: Bernkop-Schnürch
mesh_terms: D000284:Administration, Oral; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers; D004355:Drug Stability; D004789:Enzyme Activation; D041981:Gastrointestinal Tract / Q000378:metabolism*; D006801:Humans; D007408:Intestinal Absorption; D008055:Lipids / Q000737:chemistry; D053758:Nanoparticles / Q000737:chemistry*; D010539:Permeability; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D011108:Polymers / Q000737:chemistry; D012995:Solubility; D013499:Surface Properties
chemical_list: D004337:Drug Carriers; D008055:Lipids; D004364:Pharmaceutical Preparations; D011108:Polymers
keywords: liposomes; mucopenetrating nanoparticles; nanocarriers; oral drug delivery; polymeric micelles; polymeric nanoparticles; pre-uptake metabolism; self-emulsifying drug delivery systems; solid lipid nanoparticles