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水溶性聚合物骨靶向给药系统的合成与评价

Synthesis and evaluation of water-soluble polymeric bone-targeted drug delivery systems.

作者信息

Wang Dong, Miller Scott, Sima Monika, Kopecková Pavla, Kopecek Jindrich

机构信息

Department of Pharmaceutics and Pharmaceutical Chemistry/CCCD, University of Utah, Salt Lake City, Utah 84112, USA.

出版信息

Bioconjug Chem. 2003 Sep-Oct;14(5):853-9. doi: 10.1021/bc034090j.

Abstract

Four polymeric bone-targeting conjugates were synthesized based on poly(ethylene glycol) (PEG, two conjugates) and poly[N-(2-hydroxypropyl)methacrylamide] (PHPMA, two conjugates). The well-known bone-targeting compounds, alendronate and aspartic acid peptide, were used as bone-targeting moieties. Fluorescein isothiocyanate (FITC) was attached to the conjugates as a model drug for detection purposes. The bone-targeting potential of these conjugates was tested in vitro with hydroxyapatite (HA) and in mice. The data obtained indicated that these novel delivery systems could specifically accumulate in the bone tissue.

摘要

基于聚乙二醇(PEG,两种缀合物)和聚[N-(2-羟丙基)甲基丙烯酰胺](PHPMA,两种缀合物)合成了四种聚合物骨靶向缀合物。使用著名的骨靶向化合物阿仑膦酸盐和天冬氨酸肽作为骨靶向部分。异硫氰酸荧光素(FITC)作为用于检测目的的模型药物连接到缀合物上。这些缀合物的骨靶向潜力在体外使用羟基磷灰石(HA)并在小鼠体内进行了测试。获得的数据表明,这些新型递送系统可以特异性地在骨组织中积累。

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