title: Bioadhesion and enhanced bioavailability by wheat germ agglutinin-grafted lipid nanoparticles for oral delivery of poorly water-soluble drug bufalin.
abstract: Wheat germ agglutinin (WGA)-grafted lipid nanoparticles has been prepared and its in vitro association with Caco-2 cells has been studied previously. The purpose of this study was to further investigate the potential of WGA-grafted lipid nanoparticles for oral delivery of bufalin, a poorly water soluble drug, by evaluating its ex vivo bioadhesion with intestinal mucosal segments and in vivo bioavailability. A significant higher adhesion between WGA-grafted lipid nanoparticles and intestinal mucosa was found compared with that of WGA-free lipid nanoparticles (p<0.05). The in vivo pharmacodynamic studies were performed by oral administration of WGA-grafted lipid nanoparticles and suspensions to fasted rats. Compared with suspensions, WGA-grafted lipid nanoparticles showed much larger AUC and C(max), and a 2.7-fold improvement in oral bioavailability. These results illustrate the potential utility of WGA-grafted lipid nanoparticles for oral delivery of a poorly water-soluble drug such as bufalin.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201003, PR China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Liu
authors.forename: Pengfei
authors.initials: P
authors.lastname: Wang
authors.forename: Chen
authors.initials: C
authors.lastname: Sun
authors.forename: Jihui
authors.initials: J
authors.lastname: Zhao
authors.forename: Yang
authors.initials: Y
authors.lastname: Du
authors.forename: Feng
authors.initials: F
authors.lastname: Shi
authors.forename: Nianping
authors.initials: N
authors.lastname: Feng
mesh_terms: D000268:Adhesiveness; D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D001682:Biological Availability; D002018:Bufanolides / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems; D007413:Intestinal Mucosa / Q000378:metabolism; D008055:Lipids / Q000737:chemistry; D008297:Male; D053758:Nanoparticles; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013535:Suspensions; D014909:Wheat Germ Agglutinins / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D002018:Bufanolides; D008055:Lipids; D013535:Suspensions; D014909:Wheat Germ Agglutinins; C022777:bufalin