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羟基磷灰石功能化触发利塞膦酸钠的吸附和释放。

Hydroxyapatite functionalization to trigger adsorption and release of risedronate.

机构信息

Department of Chemistry "G. Ciamician", University of Bologna, via Selmi 2, 40126 Bologna, Italy.

CIRIMAT, INPT-CNRS-UPS, Université de Toulouse, Université Paul Sabatier, 4 allée Emile Monso, 31030 Toulouse cedex 4, France.

出版信息

Colloids Surf B Biointerfaces. 2017 Dec 1;160:493-499. doi: 10.1016/j.colsurfb.2017.09.055. Epub 2017 Sep 28.

Abstract

Bisphosphonates are widely employed drugs for the treatment of pathologies characterized by excessive bone resorption, and display a great affinity for apatitic supports. In this work we investigate how hydroxyapatite functionalization can influence the processes of adsorption and release of a bisphosphonate, namely risedronate. To this aim, pure hydroxyapatite (HA), hydroxyapatite with a partial substitution of Zn to Ca (ZnHA) and poly-ethylenimine-functionalized hydroxyapatite (HAPEI) were submitted to interaction with risedronate solution. The results indicate that the mechanisms of adsorption and release are greatly influenced by the type of the apatitic support. All the apatitic supports display Langmuir isotherms for risedronate adsorption. However in the case of HAPEI the plateau is not reached even at high equilibrium concentrations in solution. The data suggest that risedronate adsorption on HAPEI mineral-organic support occurs not only through chemisorption on apatitic phase, as on HA and ZnHA, but also through physisorption involved by PEI coating, which modulates also bisphosphonate release. These properties of tailor-made hydroxyapatite supports could be exploited to develop delivery systems for antiresorptive agents directly on osteoporotic sites.

摘要

双膦酸盐被广泛用于治疗骨质吸收过度相关的疾病,对磷灰石载体具有很强的亲和力。在这项工作中,我们研究了羟基磷灰石的功能化如何影响双膦酸盐(即利塞膦酸钠)的吸附和释放过程。为此,我们将纯羟基磷灰石(HA)、部分钙被锌取代的羟基磷灰石(ZnHA)和聚乙烯亚胺功能化的羟基磷灰石(HAPEI)与利塞膦酸钠溶液进行了相互作用。结果表明,吸附和释放的机制受到磷灰石载体类型的极大影响。所有的磷灰石载体都显示出利塞膦酸钠吸附的 Langmuir 等温线。然而,在 HAPEI 的情况下,即使在溶液中的平衡浓度很高时,也未达到平台。数据表明,利塞膦酸钠在 HAPEI 矿物-有机载体上的吸附不仅通过与磷灰石相的化学吸附发生,如在 HA 和 ZnHA 上,而且还通过涉及 PEI 涂层的物理吸附发生,这也调节了双膦酸盐的释放。这些定制的羟基磷灰石载体的特性可用于在骨质疏松部位直接开发抗吸收剂的输送系统。

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