In vitro evaluation of biodegradable microspheres with surface-bound ligands

In vitro evaluation of biodegradable microspheres with surface-bound ligands
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DOI:
10.1016/j.jconrel.2005.11.004
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发表时间:
2006-02-21
影响因子:
10.8
通讯作者:
Saltzman, WM
Saltzman, WM
中科院分区:
医学1区
文献类型:
--
作者:
Keegan, ME;Royce, SM;Saltzman, WM

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将蛋白质配体偶联到生物可降解微球的表面。然后将这些微球-配体缀合物用于两个体外模型系统中,以评估缀合的配体对微球行为的影响。微球保留在琼脂糖柱中增加了特异性受体的琼脂糖基质上的微球表面上的配体。在另一个实验中,与对照微球相比,将凝集素荆豆凝集素1缀合至微球表面增加了微球对Caco-2单层的粘附。这种微球粘附的增加被共同施用L-岩藻糖所抵消,表明粘附的增加是由于配体与细胞表面上的碳水化合物受体的特异性相互作用。这些结果表明,与微球缀合的配体保持其受体结合活性,并且以足以使微球靶向单层和携带互补受体的三维基质的密度存在于微球表面上。(C)2005 Elsevier B. V.保留所有权利。
Protein ligands were conjugated to the surface of biodegradable microspheres. These microsphere-ligand conjugates were then used in two in vitro model systems to evaluate the effect of conjugated ligands on microsphere behavior. Microsphere retention in agarose columns was increased by ligands on the microsphere surface specific for receptors on the agarose matrix. In another experiment, conjugating the lectin Ulex europaeus agglutinin 1 to the microsphere surface increased microsphere adhesion to Caco-2 monolayers compared to control microspheres. This increase in microsphere adhesion was negated by co-administration of L-fucose, indicating that the increase in adhesion is due to specific interaction of the ligand with carbohydrate receptors on the cell surface. These results demonstrate that the ligands conjugated to the microspheres maintain their receptor binding activity and are present on the microsphere surface at a density sufficient to target the microspheres to both monolayers and three-dimensional matrices bearing complementary receptors. (C) 2005 Elsevier B.V. All rights reserved.