title: Proliposomes containing a bile salt for oral delivery of Ginkgo biloba extract: Formulation optimization, characterization, oral bioavailability and tissue distribution in rats.
abstract: Proliposomes containing a bile salt were developed to improve the oral bioavailability of Ginkgo biloba extract (GbE). GbE loaded proliposomes (P-GbE) were successfully prepared by spray drying method. The formulation was optimized using the response surface methodology. FE-SEM, DSC, and FT-IR were used to study the surface morphology and molecular state of proliposomes, and demonstrated key interactions between the formulation ingredients. In vitro studies showed delayed release and enhanced dissolution of Ginkgo flavonoids and terpene lactones from GbE proliposomes. Proliposomes significantly enhanced GbE absorption in the gastrointestinal tract and decreased its elimination. The bioavailabilities of quercetin, kaempferol, isorhmnetin, ginkgolide A, ginkgolide B and ginkgolide C from proliposomes relative to the control were 245%, 211%, 264%, 203%, 333%, and 294%, respectively. Proliposomes were shown to selectively deliver GbE to critical target tissues. In conclusion, development of proliposomes formulation for GbE solved the problem of its poor oral bioavailability, prolonged its duration of action, and increased drug distribution in critical tissues, especially in the brain, therefore, warrant further investigation.
authors.affiliation: College of Life Sciences, Jilin University, Changchun, Jilin 130012, China.
authors.forename: Bin
authors.initials: B
authors.lastname: Zheng
authors.affiliation: College of Life Sciences, Jilin University, Changchun, Jilin 130012, China.
authors.forename: Lirong
authors.initials: L
authors.lastname: Teng
authors.affiliation: College of Life Sciences, Jilin University, Changchun, Jilin 130012, China.
authors.forename: Gaoyang
authors.initials: G
authors.lastname: Xing
authors.affiliation: College of Life Sciences, Jilin University, Changchun, Jilin 130012, China.
authors.forename: Ye
authors.initials: Y
authors.lastname: Bi
authors.affiliation: College of Life Sciences, Jilin University, Changchun, Jilin 130012, China.
authors.forename: Shuang
authors.initials: S
authors.lastname: Yang
authors.affiliation: College of Life Sciences, Jilin University, Changchun, Jilin 130012, China.
authors.forename: Fei
authors.initials: F
authors.lastname: Hao
authors.affiliation: College of Life Sciences, Jilin University, Changchun, Jilin 130012, China.
authors.forename: Guodong
authors.initials: G
authors.lastname: Yan
authors.affiliation: College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
authors.forename: Xinmei
authors.initials: X
authors.lastname: Wang
authors.affiliation: College of Life Sciences, Jilin University, Changchun, Jilin 130012, China; College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Lee
authors.affiliation: College of Life Sciences, Jilin University, Changchun, Jilin 130012, China.
authors.forename: Lesheng
authors.initials: L
authors.lastname: Teng
authors.affiliation: College of Life Sciences, Jilin University, Changchun, Jilin 130012, China. Electronic address: xiejing@jlu.edu.cn.
authors.forename: Jing
authors.initials: J
authors.lastname: Xie
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001647:Bile Acids and Salts / Q000737:chemistry*; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D020441:Ginkgo biloba / Q000737:chemistry*; D006207:Half-Life; D008081:Liposomes; D008297:Male; D008855:Microscopy, Electron, Scanning; D010936:Plant Extracts / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D017550:Spectroscopy, Fourier Transform Infrared; D014018:Tissue Distribution
chemical_list: D001647:Bile Acids and Salts; D008081:Liposomes; D010936:Plant Extracts
keywords: Ginkgo biloba extract; Oral bioavailability; Proliposomes; Response surface methodology; Tissue distribution