A new application of monosialotetrahexosylganglioside in pharmaceutics: preparation of freeze-thaw-resistant coenzyme Q10 emulsions.

Research on intravenous emulsions has been ongoing for several decades, and their unique advantages bring many opportunities for insoluble drugs. However, emulsions cannot withstand freezing in practical applications because their quality is severely affected. In this study, we used coenzyme Q10 as a model drug to prepare emulsions. Monosialotetrahexosylganglioside (GM1) was used to modify the emulsion to solve the freeze-thaw intolerance problem. The particle size, sterilization and freeze-thaw stability were affected by the oil content, phospholipid content, drug loading and homogenization conditions, which showed significant effects on the preparation properties. Emulsions prepared with a high oil content (30%, W/V) withstood three freeze-thaw cycles when the GM1 content was 0.2%-1.0% (W/V). In addition, pharmacokinetic studies indicated that emulsions modified with high-density GM1 had a long circulation time. Compared with the coenzyme Q10 solution, the emulsions showed different degrees of heart, liver, spleen and brain targeting. The relative uptake rate of the 0.2% GM1-modified emulsion in the heart was 37.06, while that of the 1.0% GM1-modified emulsion in the brain was 17.43. These results strongly suggest that coenzyme Q10 emulsions coated with GM1 can tolerate freeze-thaw cycles and are excellent for treatment of cardiac and neurodegenerative diseases. Copyright © 2021 Elsevier B.V. All rights reserved.

Citation

Yu Wang, Chunling Wang, Yihui Deng, Yanzhi Song. A new application of monosialotetrahexosylganglioside in pharmaceutics: preparation of freeze-thaw-resistant coenzyme Q10 emulsions. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2021 Apr 01;159:105701

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PMID: 33429046

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