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近年来双膦酸盐类药物在骨相关疾病中的应用得到广泛关注。由于其特殊的分子结构,在体内不易水解,对骨组织中的无机物羟基磷灰石有较高的亲和力,因此双膦酸盐类药物在骨相关疾病的治疗和诊断中都发挥着重要的作用。随着医疗材料的发展,双膦酸盐功能化纳米载体作为骨靶向载体可为双膦酸盐在骨相关疾病中的应用提供更好的方案。笔者在本文中从双膦酸盐的分子结构到其主要的临床应用做了相关综述。
双膦酸盐在骨相关疾病诊断和治疗中的研究进展
Advances in the diagnosis and treatment of bone related diseases by bisphosphonates
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摘要: 双膦酸盐是目前治疗骨代谢性疾病中重要的一类抗骨吸收药物,主要运用于Paget's病、骨质疏松症和肿瘤相关性骨病。双膦酸盐类药物已广泛应用于骨相关疾病的治疗中,双膦酸盐类功能化显像剂在核医学骨显像中也被广泛应用。放射性示踪剂可通过螯合作用与双膦酸盐偶联,偶联后的探针作为骨靶向的示踪剂应用于骨显像。双膦酸盐的分子结构中含有P-C-P键,在人体内不易被酶水解。因其与骨组织中的无机物羟基磷灰石晶体有较高的亲和力,故在骨组织中有较高的选择性沉积。基于双膦酸盐的一般特征和作用机制,笔者概述了双膦酸盐功能显像剂、骨质疏松的治疗和双膦酸盐应用于骨转移治疗的临床前研究。Abstract: Bisphosphonate is one of the important antibone absorbents in the treatment of bone metabolic diseases. It is mainly used in Paget's disease, osteoporosis and bone disease associated with tumor. Bisphosphonates are not only used to treat bone-related diseases, but bisphosphonate functionalized imaging agents are widely used in the diagnosis of bone-related diseases in nuclear medical bone imaging. The radioactive tracer can be coupled with bisphosphonates by chelation, and the coupled probe can be used as a bone targeting tracer for bone imaging. The molecular structure of bisphosphonates contains P-C-P bonds, so they are resistant to enzymatic hydrolysis and are not easily hydrolyzed by enzymes in human body. Because of its high affinity with inorganic hydroxyapatite crystals in bone tissue, it has high selectivity in bone tissue. This paper is based on the general characteristics and mechanism of bisphosphonates and summarized the preclinical study on the treatment of osteoporosis with bisphosphonates and the application of bisphosphonates in the treatment of bone metastasis.
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Key words:
- Biphosphonate /
- osteoporosis /
- Bone tumors /
- Bone imaging
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