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Tissue Distribution and Enhanced in Vivo Anti-Hyperlipidemic-Antioxidant Effects of Perillaldehyde-Loaded Liposomal Nanoformulation Against Poloxamer 407-induced Hyperlipidemia

Tissue Distribution and Enhanced in Vivo Anti-Hyperlipidemic-Antioxidant Effects of Perillaldehyde-Loaded Liposomal Nanoformulation Against Poloxamer 407-induced Hyperlipidemia

Emmanuel Omari-Siaw, Qilong Wang, Congyong Sun, Zengquan Gu, Yuan Zhu, Xia Cao, Caleb Kesse Firempong, Rita Agyare, Ximing Xu, Jiangnan Yu

Int J Pharm. 2016 Nov 20;513(1-2):68-77.

PMID: 27567929

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, Cmax and 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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP18031408	(S)-(−)-Perillaldehyde		18031-40-8	Price

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