Cytotoxicity evaluation of symmetrically branched glycerol trimer in human hepatocellular carcinoma HepG2 cells

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  • Miyamoto Licht
    Department of Medical Pharmacology, Institute of Health Biosciences, The University of Tokushima Graduate School Department of Pharmaceutical Chemistry, Institute of Health Biosciences, The University of Tokushima Graduate School
  • Watanabe Masashi
    Department of Medical Pharmacology, Institute of Health Biosciences, The University of Tokushima Graduate School
  • Kono Mai
    Department of Medical Pharmacology, Institute of Health Biosciences, The University of Tokushima Graduate School
  • Matsushita Tsuyoshi
    Department of Pharmaceutical Chemistry, Institute of Health Biosciences, The University of Tokushima Graduate School
  • Hattori Hatsuhiko
    Department of Pharmaceutical Chemistry, Institute of Health Biosciences, The University of Tokushima Graduate School
  • Ishizawa Keisuke
    Department of Medical Pharmacology, Institute of Health Biosciences, The University of Tokushima Graduate School
  • Nemoto Hisao
    Department of Pharmaceutical Chemistry, Institute of Health Biosciences, The University of Tokushima Graduate School
  • Tsuchiya Koichiro
    Department of Medical Pharmacology, Institute of Health Biosciences, The University of Tokushima Graduate School

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An appropriate balance between lipophilicity and hydrophilicity is necessary for pharmaceuticals to achieve fine Absorption, Distribution, Metabolism and Excretion (ADME) properties including absorption and distribution, in particular. We have designed and proposed symmetrically branched oligoglycerols (BGL) as an alternative approach to improve the lipophilic-hydrophilic balance. We have previously shown that stability in circulation and water-solubility of such molecules as proteins, liposomes and hydrophobic compounds are much improved by conjugation to BGL. Albeit these successful applications of BGL, little was known whether BGL could be used in safety. Thus we conducted evaluation of the cytotoxicity of a representative BGL, symmetrically branched glycerol trimer (BGL003) in the cultured cells to clarify its biological safeness. Here we demonstrate that water-solubility of an extremely hydrophobic agent, fenofibrate was more than 2,000-fold improved just by conjugated with BGL003. BGL003 did not exhibit any significant cytotoxicity in human hepatocarcinoma HepG2 cells. Thus BGL003 should be safe and suitable strategy to endow hydrophobic molecules with much hydrophilicity.

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