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Preparation and Preclinical Evaluation of Intravenous Lipid Emulsion Containing a Novel Thiochromanone Derivative (CF) with Low Toxicity

Asian Journal of Pharmaceutical and Health Sciences,2016,6,2,1429-1433.
Published:June 2016
Type:Research Article
Authors:
Author(s) affiliations:

Liandong Hu1,2*, Saixi Pang1,2, Peishan Li1,2, Yaxing Zhao1,2, Qiaofeng Hu1,2, Dongqian Kong1,2, Xiaoyun Xiong3, Jianying Su3

1School of Pharmaceutical Sciences, Hebei University, Baoding 071002, China.

2Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding 071002, China.

3Xi'an Lijun Pharmaceutical Co., Xian, 710000, China.

Abstract:

In this study, (Z)-3-(chloromethylene)-6-fluorothiochroman-4- one (CF), a novel thiochromanone derivative was organized. Lipid emulsion containing CF (CF-LE) was developed by high pressure homogenization to improve its solubility. The physicochemical properties such as morphology, particle size, zeta potential and yielding efficiency of CF-LE were studied. Stability and safety assessment (including hemolytic test, vascular irritation test and paw lick test) of CF-LE was also investigated. The optimum CF-LE, consisting of 10% MCT, 1.2% egg yolk lecithin, 0.6% F68, 0.4% oleic acid and 2.25% glycerol, was prepared at 800 bar for 10 cycles. The average particle size of CF-LE was 234.7nm, z-potential was -30.76 mV, and entrapment efficiency was 95%. CF-LE showed a sufficient physicochemical stability in the long-term centrifugation and dilution with 0.9% sodium chloride injection and 5% glucose injection for 6 h. It did not cause any hemolysis and blood coagulation in vitro and did not cause obvious intravenous irritation. The results suggested that CF-LE was a promising drug delivery system for CF intravenous administration.

Micrograph of CF-LE