Hydroxyapatite crystals as a local delivery system for cisplatin: adsorption and release of cisplatin in vitro
Hydroxyapatite crystals as a local delivery system for cisplatin: adsorption and release of cisplatin in vitro
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DOI：
10.1016/s0736-0266(01)00105-x
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发表时间：
2002-03-01
影响因子：
2.8
通讯作者：
Glimcher, MJ
中科院分区：
文献类型：
--
作者：
Barroug, A;Glimcher, MJ
本研究描述了在体外结合和释放的抗肿瘤药物顺铂的合成羟基磷灰石晶体在水介质中进行的浆料的特性。顺铂的吸附羟基磷灰石浆料和其释放被发现显着依赖于所使用的水性介质的离子组成。在恒定的pH值7.4下。与来自含有氯离子的磷酸盐缓冲溶液相比，来自无氯磷酸盐缓冲溶液或Tris缓冲溶液的浆液中的羟基磷灰石晶体吸附了显著更多的顺铂。羟基磷灰石结合的顺铂解吸到溶液中的量也逐渐增加，作为平衡溶液中氯化物浓度增加的函数。在Tris或磷酸盐缓冲液中，很少有羟基磷灰石结合的顺铂从晶体中释放。这些结果表明，它是顺铂的水合衍生物，这是参与吸附顺铂的羟基磷灰石晶体。吸附数据可以表示为Freundlich等温线，从该等温线可以计算缔合常数。即使在磷酸盐缓冲液中氯离子的最大浓度下，与羟基磷灰石晶体结合的顺铂的释放速率也相对较慢。在4.25天后，约33%的与羟基磷灰石晶体结合的总顺铂被释放。在用新鲜缓冲液额外平衡两周后，释放另外15%的与羟基磷灰石晶体结合的剩余顺铂（最初结合的总顺铂的58%）。这些发现表明，顺铂结合到浆的羟基磷灰石晶体可能是有用的恶性肿瘤的局部治疗。(C)2002骨科研究学会。由爱思唯尔科技有限公司出版。保留所有权利。
This study describes the characteristics of the in vitro binding and release of the anti-tumor drug cisplatin by slurries of synthetic hydroxyapatite crystals carried out in aqueous media. The adsorption of cisplatin by slurries of hydroxyapatite and its release were found to depend significantly on the ionic composition of the aqueous media used. At a constant pH of 7.4. significantly more cisplatin is adsorbed by the hydroxyapatite crystals in the slurry from a chloride-free phosphate buffered solution or a Tris buffered solution than from a buffered phosphate solution containing chloride ions. The amount of hydroxyapatite-bound cisplatin desorbed into solution was also progressively increased as a function of the increasing concentration of chloride in the equilibrating solution. Very little hydroxyapatite-bound cisplatin was released from the crystals in either a Tris or phosphate buffer. These results suggest that it is the hydrated derivatives of cisplatin which are involved in the adsorption of cisplatin by hydroxyapatite crystals. The adsorption data can be expressed as a Freundlich isotherm from which the association constant can be calculated, The rate of release of cisplatin bound to crystals of hydroxyapatite is relatively slow even at the maximum concentration of chloride ions in the phosphate buffer. Approximately 33% of the total cisplatin bound to the crystals of hydroxyapatite was released after 4.25 days. An additional 15% of the remaining cisplatin bound to the hydroxyapatite cyrstals was released after an additional equilibration with fresh buffer for two weeks (58% of the total cisplatin originally bound). These findings Suggest that cisplatin bound to slurries of hydroxyapatite crystals may be useful in the local treatment of malignant tumors. (C) 2002 Orthopaedic Research Society. Published by Elsevier Science Ltd. All rights reserved.