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Hypolipidemic Potential of Perillaldehyde-Loaded Self-Nanoemulsifying Delivery System in High-Fat Diet Induced Hyperlipidemic Mice: Formulation, in Vitro and in Vivo Evaluation

Hypolipidemic Potential of Perillaldehyde-Loaded Self-Nanoemulsifying Delivery System in High-Fat Diet Induced Hyperlipidemic Mice: Formulation, in Vitro and in Vivo Evaluation

Emmanuel Omari-Siaw, Yuan Zhu, Houyong Wang, Wei Peng, Caleb Kesse Firempong, Yuan Wen Wang, Xia Cao, Wenwen Deng, Jiangnan Yu, Ximing Xu

Eur J Pharm Sci. 2016 Mar 31;85:112-22.

PMID: 26851382

Abstract:

This study reports the hypolipidemic effects of perillaldehyde-loaded self-nanoemulsifying delivery system (PAH-SNEDS) developed with D-optimal experimental design based on a three component system: 40% w/w drug-oil phase, X1 (a mixture of perillaldehyde-isopropyl myristate/medium chain triglyceride, 1:1, w/w); 48% surfactant, X2 (Kolliphor EL); and 12% co-surfactant, X3 (PEG 200). The design space was navigated using a linear model to produce spherical and homogenous droplets which were observed under TEM, with mean size, polydispersity index (PDI) and zeta potential of 32.8 ± 0.1 nm, 0.270 ± 0.029 and -10.14 ± 0.66 mV, respectively. PAH-SNEDS demonstrated significant increase in dissolution in vitro compared to the free PAH, and further yielded an oral relative bioavailability of about 206.18% in vivo which suggested a promising formulation design for potential liquid bioactive compounds. Oral administration of PAH-SNEDS (240 mg/kg per body weight) in high-fat induced hyperlipidemia in mice, also significantly decreased serum total cholesterol (TC), triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C) while increasing high-density lipoprotein cholesterol (HDL-C) level. The improved bioavailability and functional application of PAH via SNEDDS suggested a suitable approach to promote hypolipidemic effect of the drug. Perillaldehyde, therefore, promises to be a useful bioactive compound to prevent high-fat diet induced hyperlipidemia.

Chemicals Related in the Paper:

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

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