title: Enhanced oral bioavailability and in vivo antioxidant activity of chlorogenic acid via liposomal formulation.
abstract: In the present study, a formulation system consisting of cholesterol and phosphatidyl choline was used to prepare an effective chlorogenic acid-loaded liposome (CAL) with an improved oral bioavailability and an increased antioxidant activity. The developed liposomal formulation produced regular, spherical and multilamellar-shaped distribution nanoparticles. The pharmacokinetic analysis of CAL compared with chlorogenic acid (CA), showed a higher value of Cmax(6.42 ± 1.49 min versus 3.97 ± 0.39 min) and a delayed Tmax(15 min versus 10 min), with 1.29-fold increase in relative oral bioavailability. The tissue distribution in mice also demonstrated that CAL predominantly accumulated in the liver which indicated hepatic targeting potential of the drug. The increased activities of antioxidant enzymes (Total Superoxide Dismutase (T-SOD) and Glutathione Peroxidase (GSH-Px)) and total antioxidant capacity (T-AOC), in addition to decreased level of malondialdehyde (MDA) in CCl4-induced hepatotoxicity study further revealed that CAL exhibited significant hepatoprotective and antioxidant effects. Collectively, these findings present a liposomal formulation with significantly improved oral bioavailability and an increased in vivo antioxidant activity of CA.
authors: Center for Nano Drug/Gene Delivery and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang 212013, China.
authors: Yingshu
authors: Y
authors: Feng
authors: Center for Nano Drug/Gene Delivery and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang 212013, China.
authors: Congyong
authors: C
authors: Sun
authors: Center for Nano Drug/Gene Delivery and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang 212013, China.
authors: Yangyang
authors: Y
authors: Yuan
authors: Center for Nano Drug/Gene Delivery and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang 212013, China.
authors: Yuan
authors: Y
authors: Zhu
authors: Center for Nano Drug/Gene Delivery and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang 212013, China.
authors: Jinyi
authors: J
authors: Wan
authors: Center for Nano Drug/Gene Delivery and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang 212013, China.
authors: Caleb Kesse
authors: CK
authors: Firempong
authors: Center for Nano Drug/Gene Delivery and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang 212013, China.
authors: Emmanuel
authors: E
authors: Omari-Siaw
authors: Center for Nano Drug/Gene Delivery and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang 212013, China.
authors: Yang
authors: Y
authors: Xu
authors: Center for Nano Drug/Gene Delivery and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang 212013, China.
authors: Zunqin
authors: Z
authors: Pu
authors: Center for Nano Drug/Gene Delivery and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang 212013, China. Electronic address: yjn@ujs.edu.cn.
authors: Jiangnan
authors: J
authors: Yu
authors: Center for Nano Drug/Gene Delivery and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang 212013, China. Electronic address: xmxu@ujs.edu.cn.
authors: Ximing
authors: X
authors: Xu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D001682:Biological Availability; D002251:Carbon Tetrachloride; D056486:Chemical and Drug Induced Liver Injury / Q000097:blood / Q000188:drug therapy / Q000378:metabolism; D002726:Chlorogenic Acid / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D002784:Cholesterol / Q000737:chemistry; D005979:Glutathione Peroxidase / Q000097:blood / Q000378:metabolism; D008081:Liposomes; D008297:Male; D008315:Malondialdehyde / Q000097:blood / Q000378:metabolism; D051379:Mice; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry / Q000627:therapeutic use; D017207:Rats, Sprague-Dawley; D013482:Superoxide Dismutase / Q000097:blood / Q000378:metabolism
chemical_list: D000975:Antioxidants; D008081:Liposomes; D002726:Chlorogenic Acid; D008315:Malondialdehyde; D002784:Cholesterol; D002251:Carbon Tetrachloride; D005979:Glutathione Peroxidase; D013482:Superoxide Dismutase
keywords: Antioxidant activity; Bioavailability; Chlorogenic acid; Hepatoprotective; Liposome