シアル酸修飾による糖蛋白質結合リポソームの細網内皮系(RES)への取り込み抑制と促進に関する検討  [in Japanese] Reduction and increase of the reticuloendotherial system(RES) uptake of glycoprotein-conjugated liposomes by linking a ternimal sugar-chain with sialic acid.  [in Japanese]

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Author(s)

    • 小島 周二 KOJIMA Shuji
    • 東京理科大学薬学部放射薬品化学 Department of Radiochemistry, Faculty of Pharmaceutical Sciences, Tokyo University of Science
    • 曽川 裕介 SIGAWA Yusuke
    • 東京理科大学薬学部放射薬品化学 Department of Radiochemistry, Faculty of Pharmaceutical Sciences, Tokyo University of Science
    • 田尻 芳香 TAJIRI Yosika
    • 東京理科大学薬学部放射薬品化学 Department of Radiochemistry. Faculty of Pharmaceutical Sciences, Tokyo University of Science
    • 山嵜 登 YAMAZAKI Noboru
    • 産業技術総合研究所ナノテクノロジー Nanotechnology Research Institute, National Institute of Advanced Industrial Science and Technology

Abstract

Different sialic acid-linked glycoprotein-conjuagted liposomes were prepared. <I>N</I>-acetyl-glacosaminylated (GlcNAc) human albumin (HSA)-coupled iposomes (GlcNAc-HSA-Lip) were enzymatically galactosylated at 4-position, and fucosylated at 3-position of GlcNAc to prepare LX. Galactose of LX was enzymatically sialylated at 3-position to do SLX. GlcNAc of GlcNAc-HSA-Lip was modified with 3'-sialyated galactose, or 6'-sialyated galactose at 4-position, to prepare 3 SLN and 6 SLN, respectively. The reticuloendotherial system (RES) uptake of these conjugates was investigated in Ehrlich-solid tumor-bearing mice. Sialic acid linked with a terminal sugar chain of SLX increased the uptake by RES, such as liver and spleen. Whereas, sialic acid of 3 SLN and 6 SLN reduced the RES uptake. Besides, uptake of liposomes by tumor tissues was closely correlated with a long blood circulating character of these conjugates. These results suggest that sialic acid residue increases the RES uptake of glycoprotein-conjugated liposomes in presence of fucose-residue nearby, while it reduces the uptake via masking galactose-residue in absence of fucose-residue. Thus, modification of glycoprotein-conjugated liposomes with sialic acid may lead to be development of a useful carrier for drug delivery system (DDS).

Journal

  • Drug Delivery System

    Drug Delivery System 17(1), 63-68, 2002-01-10

    THE JAPAN SOCIETY OF DRUG DELIVERY SYSTEM

References:  19

Codes

  • NII Article ID (NAID)
    10008132113
  • NII NACSIS-CAT ID (NCID)
    AN10084591
  • Text Lang
    JPN
  • Article Type
    ART
  • ISSN
    09135006
  • Data Source
    CJP  J-STAGE 
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