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Hepatocellular Targeted α-Tocopherol based pH sensitive Galactosylated Lipid: Design, Synthesis and Transfection Studies

Abstract

Receptor mediated gene delivery to liver offers advantages in treating genetic disorders such as hemophilia, hereditary tyrosinemia type I (HTI). Prior findings demonstrated that tethering D-Galactose head group to cationic lipids direct genes to liver via asialo-glycoprotein receptors (ASGPR). In our continued efforts for developing safer and efficient lipofectins, we demonstrated that cationic lipids bearing α-tocopherol, an antioxidant as a hydrophobic domain could be able to deliver genes efficiently with high safety profiles in multiple cell lines. Towards developing ASGPR targeted pH sensitive cationic lipid, we have designed galactosylated cationic lipid (Toc-Gal) with α-tocopherol as hydrophobic core covalently connected with pH responsive triazole moiety and a non-targeting control lipid (Toc-OH) without galactose head group. In this study, we present design and synthesis of pH sensitive galactosylated cationic lipid (Toc-Gal), comparative transfection biology, cellular uptake studies, serum stability and cytotoxicity profiles in both ASGPR positive and negative liver cells i.e. HepG2 and SK-Hep-1 respectively.

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Publication details

The article was received on 08 Oct 2017, accepted on 05 Dec 2017 and first published on 06 Dec 2017


Article type: Research Article
DOI: 10.1039/C7MD00503B
Citation: Med. Chem. Commun., 2017, Accepted Manuscript
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    Hepatocellular Targeted α-Tocopherol based pH sensitive Galactosylated Lipid: Design, Synthesis and Transfection Studies

    S. V. Patri, V. Muripiti, B. Lohchania and S. K. Marepally, Med. Chem. Commun., 2017, Accepted Manuscript , DOI: 10.1039/C7MD00503B

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