Evaluation of pentaerythritol-based and trimethylolpropane-based cationic lipidic materials for gene delivery.

Shuang Wu, Meiyan Liu, Xiang Hu, Chengxi He, Chunyan Zhao, Shuanglin Xiang, Youlin Zeng

Bioorganic & medicinal chemistry letters 2022 Apr 15

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The chemical and physical structure of cationic liposomes pays an important effect on their gene transfection efficiency. Investigation on the structure-function relationship of cationic liposomes will guide the design of novel cationic liposomes with high transfection efficiency and biosafety. In this paper, two novel series of lipids based on the backbone of pentaerythritol and trimethylolpropane were discovered, and their gene transfection efficiencies were assayed in vitro. The four lipids 8c, 9c, 14b, and 15b, exhibited much better transfection efficiency in the HEK293 cell lines compared with Lipo2000, lipid 9c also showed good transfection efficiency in the SW480 cell lines. And the structure-efficiency relationship revealed that a hydroxyethyl polar head group boosted transfer potency in trimethylolpropane-type lipids, but reduced in pentaerythritol-type lipids. Copyright © 2022 Elsevier Ltd. All rights reserved.

Citation

Shuang Wu, Meiyan Liu, Xiang Hu, Chengxi He, Chunyan Zhao, Shuanglin Xiang, Youlin Zeng. Evaluation of pentaerythritol-based and trimethylolpropane-based cationic lipidic materials for gene delivery. Bioorganic & medicinal chemistry letters. 2022 Apr 15;62:128635