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Improved performance by replacing iminodiacetic residues with glyceryl residues in symmetrically branched oligoglycerols |
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| Authors: | Nemoto Hisao Ishihara Atsushi Araki Takaaki Katagiri Ayato Kamiya Masaki Matsushita Tsuyoshi Hattori Hatsuhiko Mimura Yukiteru Tomoda Yutaka Yamasaki Motoo |
| Affiliation: | a Department of Pharmaceutical Chemistry, Institute of Health Biosciences, Graduate School of The University of Tokushima, 1-78-1 Sho-machi, Tokushima 770-8505, Japan b Drug Formulation Research and Development Laboratories, Production Division, Kyowa Hakko Kirin Co., Ltd, 1188 Shimotogari, Nagaizumi-cho, Sunto-gun, Shizuoka 411-8731, Japan c Innovative Drug Research Laboratories, Research Division, Kyowa Hakko Kirin Co., Ltd, 3-6-6 Asahi-machi, Machida, Tokyo 194-8533, Japan |
| Abstract: | Synthesis of a symmetrically branched diglycerol (BGL002, involving one iminodiacetic residue) as a G2 dendron, and the tetradecaglycerol (BGL014, involving one iminodiacetic residue) as a G4 dendron, is described. Several members of the BGL family of G2-G4 dendrons were assembled, with G2 bearing four hydroxyl groups at the terminus region, G3 bearing eight, and G4 bearing sixteen. It is noteworthy that triglycerol (BGL003, including no iminodiacetic residue), has a water-solubility ten times higher than BGL002, and the liposome surrounded by BGL014 has a duration period in blood vessel roughly two times longer than the liposome surrounded by dodecaglycerol (BGL012, including three iminodiacetic residues). |
| Keywords: | Symmetrically branched oligoglycerols Dendron Water-solubility Liposome Duration period |
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