title: Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems: in vitro, in vivo and in situ intestinal permeability studies.
abstract: The main purpose of this work was to develop and evaluate a self-emulsifying drug delivery system (SEDDS) of piperine to enhance its solubility and bioavailability. The formulation was optimized by solubility test and ternary phase diagrams. Then physiochemical properties and in vitro release of SEDDS were characterized. In vivo pharmacokinetics study and in situ single-pass intestinal perfusion were performed to investigate the effects of SEDDS on the bioavailability and intestinal absorption of piperine. The optimized formulation was composed of ethyl oleate, Tween 80 and Transcutol P (3:5.5:1.5, w/w), with the level of the piperine reached 2.5% (w/w). The in vitro dissolution rates of piperine SEDDS were significantly higher than the self-prepared capsules. In vivo pharmacokinetic study showed Cmax1, Cmax2 and area under the curve of piperine after oral administration of SEDDS in rats were 3.8-, 7.2- and 5.2-fold higher than the self-prepared capsules, respectively, and the relative bioavailability of SEDDS was 625.74%. The in situ intestinal absorption study revealed that the effective permeability and the effective absorption rate values of piperine for SEDDS were significantly improved comparing to solutions (p < 0.01). So SEDDS formulation could improve the oral bioavailability and intestinal absorption of piperine effectively.
authors.affiliation: a Department of Pharmacy, The Second Affiliated Hospital , Harbin Medical University, Key Laboratory of medications research, College of Heilongjiang Province , Harbin , P. R. China and.
authors.forename: Bing
authors.initials: B
authors.lastname: Shao
authors.affiliation: a Department of Pharmacy, The Second Affiliated Hospital , Harbin Medical University, Key Laboratory of medications research, College of Heilongjiang Province , Harbin , P. R. China and.|b Department of Pharmaceutics, School of Pharmacy , Harbin Medical University , Harbin , P. R. China.
authors.forename: Chao
authors.initials: C
authors.lastname: Cui
authors.affiliation: a Department of Pharmacy, The Second Affiliated Hospital , Harbin Medical University, Key Laboratory of medications research, College of Heilongjiang Province , Harbin , P. R. China and.
authors.forename: Hongyu
authors.initials: H
authors.lastname: Ji
authors.affiliation: b Department of Pharmaceutics, School of Pharmacy , Harbin Medical University , Harbin , P. R. China.
authors.forename: Jingling
authors.initials: J
authors.lastname: Tang
authors.affiliation: a Department of Pharmacy, The Second Affiliated Hospital , Harbin Medical University, Key Laboratory of medications research, College of Heilongjiang Province , Harbin , P. R. China and.
authors.forename: Zhiyong
authors.initials: Z
authors.lastname: Wang
authors.affiliation: a Department of Pharmacy, The Second Affiliated Hospital , Harbin Medical University, Key Laboratory of medications research, College of Heilongjiang Province , Harbin , P. R. China and.
authors.forename: Hongmei
authors.initials: H
authors.lastname: Liu
authors.affiliation: a Department of Pharmacy, The Second Affiliated Hospital , Harbin Medical University, Key Laboratory of medications research, College of Heilongjiang Province , Harbin , P. R. China and.
authors.forename: Mengnan
authors.initials: M
authors.lastname: Qin
authors.affiliation: a Department of Pharmacy, The Second Affiliated Hospital , Harbin Medical University, Key Laboratory of medications research, College of Heilongjiang Province , Harbin , P. R. China and.
authors.forename: Xin
authors.initials: X
authors.lastname: Li
authors.affiliation: a Department of Pharmacy, The Second Affiliated Hospital , Harbin Medical University, Key Laboratory of medications research, College of Heilongjiang Province , Harbin , P. R. China and.
authors.forename: Linhua
authors.initials: L
authors.lastname: Wu
mesh_terms: D000284:Administration, Oral; D000470:Alkaloids / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D000818:Animals; D019540:Area Under Curve; D052117:Benzodioxoles / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems / Q000379:methods*; D065546:Drug Liberation; D045703:Emulsifying Agents / Q000737:chemistry; D004655:Emulsions / Q000737:chemistry*; D007408:Intestinal Absorption; D008055:Lipids / Q000737:chemistry; D008297:Male; D010880:Piperidines / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D053284:Polyunsaturated Alkamides / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D000470:Alkaloids; D052117:Benzodioxoles; D045703:Emulsifying Agents; D004655:Emulsions; D008055:Lipids; D010880:Piperidines; D053284:Polyunsaturated Alkamides; C008922:piperine
keywords: Bioavailability; dissolution; piperine; self-emulsifying drug delivery system; single-pass intestinal perfusion