title: Tissue distribution and enhanced in vivo anti-hyperlipidemic-antioxidant effects of perillaldehyde-loaded liposomal nanoformulation against Poloxamer 407-induced hyperlipidemia.
abstract: An optimized perillaldehyde-loaded liposomal nanoformulation (PAH-LNF) was successfully applied to improve the pharmacological effect of perillaldehyde (PAH) in poloxamer 407-induced hyperlipidemia. Oral administration of PAH-LNF (240mg/kg per body weight) in rats significantly enhanced solubility and relative bioavailability (270.7%) compared to the free PAH with about 2.7-, 1.5-, 1.3-, 1.3- and 1.5-fold increase in AUC, T1/2, MRT, Cmaxand Tmax, respectively. Tissue distribution study also revealed the accumulation of PAH in the liver, lungs, spleen, kidney, brain and heart in order of decreasing affinity. Moreover, a significant decrease in serum total cholesterol (TC), triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C) with simultaneous increase in high-density lipoprotein cholesterol (HDL-C) level was observed in the chemically-induced hyperlipidemic mice which further confirmed PAH's anti-hyperlipidemic properties. Additionally, PAH-LNF also significantly increased the activities of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) with a concurrent decrease in malondialdehyde (MDA) to affirm the antioxidant and hepatoprotective effects of PAH. Thus, liposomal nanoformulation promises to be a useful drug delivery system for the development of PAH.
authors: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang 212013, People's Republic of China; Department of Pharmaceutical Sciences, Kumasi Polytechnic, P.O. Box 854, Kumasi, Ghana.
authors: Emmanuel
authors: E
authors: Omari-Siaw
authors: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang 212013, People's Republic of China.
authors: Qilong
authors: Q
authors: Wang
authors: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang 212013, People's Republic of China.
authors: Congyong
authors: C
authors: Sun
authors: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang 212013, People's Republic of China.
authors: Zengquan
authors: Z
authors: Gu
authors: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang 212013, People's Republic of China.
authors: Yuan
authors: Y
authors: Zhu
authors: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang 212013, People's Republic of China.
authors: Xia
authors: X
authors: Cao
authors: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang 212013, People's Republic of China.
authors: Caleb Kesse
authors: CK
authors: Firempong
authors: Overseas Education College, Jiangsu University, Zhenjiang 212013, People's Republic of China.
authors: Rita
authors: R
authors: Agyare
authors: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang 212013, People's Republic of China. Electronic address: xmxu@ujs.edu.cn.
authors: Ximing
authors: X
authors: Xu
authors: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang 212013, People's Republic of China; School of Pharmacy, China Pharmaceutical University, Nanjing, People's Republic of China.
authors: Jiangnan
authors: J
authors: Yu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D019540:Area Under Curve; D001682:Biological Availability; D016503:Drug Delivery Systems; D006207:Half-Life; D006949:Hyperlipidemias / Q000188:drug therapy*; D000960:Hypolipidemic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D008055:Lipids / Q000097:blood; D008081:Liposomes; D008297:Male; D051379:Mice; D039821:Monoterpenes / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D053758:Nanoparticles; D020442:Poloxamer / Q000633:toxicity; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013482:Superoxide Dismutase / Q000378:metabolism; D014018:Tissue Distribution
chemical_list: D000975:Antioxidants; D000960:Hypolipidemic Agents; D008055:Lipids; D008081:Liposomes; D039821:Monoterpenes; D020442:Poloxamer; C033342:perillaldehyde; D013482:Superoxide Dismutase
keywords: Anti-hyperlipidemic activity; Antioxidant; Liposomal nanoformulations; Perillaldehyde; Poloxamer 407