title: Oleic acid derivative of polyethylenimine-functionalized proliposomes for enhancing oral bioavailability of extract of Ginkgo biloba.
abstract: The present systematic study focused to investigate the oleic acid derivative of branched polyethylenimine (bPEI-OA)-functionalized proliposomes for improving the oral delivery of extract of Ginkgo biloba (GbE). The GbE proliposomes were prepared by a spray drying method at varying ratios of egg yolk phosphatidylcholine and cholesterol, and the optimized formulation was tailored with bPEI-OA to obtain bPEI-OA-functionalized proliposomes. The formulations were characterized for particle size, zeta potential, and entrapment efficiency. The release of GbE from proliposomes exhibited a sustained release. And the release rate was regulated by changing the amount of bPEI-OA on the proliposomes. The physical state characterization studies showed some interactions between GbE and other materials, such as hydrogen bonds and van der Waals forces during the process of preparation of proliposomes. The in situ single-pass perfusion and oral bioavailability studies were performed in rats. The significant increase in absorption constant (Ka) and apparent permeability coefficient (Papp) from bPEI-OA-functionalized proliposomes indicated the importance of positive charge for effective uptake across the gastrointestinal tract. The oral bioavailability of bPEI-OA-functionalized proliposomes was remarkable enhanced in comparison with control and conventional proliposomes. The bPEI-OA-functionalized proliposomes showed great potential of improving oral absorption of GbE as a suitable carrier.
authors.affiliation: a College of Life Science, Jilin University , Changchun , Jilin , China .
authors.forename: Bin
authors.initials: B
authors.lastname: Zheng
authors.affiliation: a College of Life Science, Jilin University , Changchun , Jilin , China .
authors.forename: Shuang
authors.initials: S
authors.lastname: Yang
authors.affiliation: a College of Life Science, Jilin University , Changchun , Jilin , China .
authors.forename: Chunyu
authors.initials: C
authors.lastname: Fan
authors.affiliation: a College of Life Science, Jilin University , Changchun , Jilin , China .
authors.forename: Ye
authors.initials: Y
authors.lastname: Bi
authors.affiliation: b The First Hospital of Jilin University , Changchun , Jilin , China .
authors.forename: Lin
authors.initials: L
authors.lastname: Du
authors.affiliation: c The Secord Hospital of Jilin University , Changchun , Jilin , China , and.
authors.forename: Lingzhi
authors.initials: L
authors.lastname: Zhao
authors.affiliation: a College of Life Science, Jilin University , Changchun , Jilin , China .|d College of Pharmacy, The Ohio State University , Columbus , OH , USA.
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Lee
authors.affiliation: a College of Life Science, Jilin University , Changchun , Jilin , China .
authors.forename: Lesheng
authors.initials: L
authors.lastname: Teng
authors.affiliation: a College of Life Science, Jilin University , Changchun , Jilin , China .
authors.forename: Lirong
authors.initials: L
authors.lastname: Teng
authors.affiliation: a College of Life Science, Jilin University , Changchun , Jilin , China .
authors.forename: Jing
authors.initials: J
authors.lastname: Xie
mesh_terms: D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D002784:Cholesterol / Q000737:chemistry* / Q000378:metabolism; D004337:Drug Carriers; D020441:Ginkgo biloba / Q000737:chemistry / Q000378:metabolism*; D008081:Liposomes; D019301:Oleic Acid / Q000737:chemistry*; D010316:Particle Size; D010539:Permeability; D010713:Phosphatidylcholines / Q000737:chemistry* / Q000378:metabolism; D011094:Polyethyleneimine / Q000737:chemistry*; D051381:Rats
chemical_list: D004337:Drug Carriers; D008081:Liposomes; D010713:Phosphatidylcholines; D019301:Oleic Acid; D011094:Polyethyleneimine; D002784:Cholesterol
keywords: Extract of Ginkgo biloba; in situ perfusion; oral bioavailability; polyethylenimine; proliposomes