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镝/钬标记的多孔羟基磷灰石微粒用于治疗炎性关节疾病——探索体内发生器的优势

Dy/Ho-labeled porous hydroxyapatite microparticles for treatment of inflammatory joint diseases - Exploring the advantages of in vivo generator.

作者信息

Patra Sourav, Singh Khajan, Chakraborty Avik, Mohammed Shahiralam Khan, Rakshit Sutapa, Chakravarty Rubel, Chakraborty Sudipta

机构信息

Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Mumbai, 400085, India.

Homi Bhabha National Institute, Anushaktinagar, Mumbai, 400094, India.

出版信息

Sci Rep. 2025 May 20;15(1):17480. doi: 10.1038/s41598-025-02373-5.

DOI:10.1038/s41598-025-02373-5
PMID:40394061
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12092808/
Abstract

Holmium-166 [T = 26.8 h, E (max) = 1.74 MeV (48.7%) and 1.85 MeV (50.0%); Eγ = 80.6 keV (10.6%)] is one of the most promising radionuclides in radiation synovectomy (RSV) for the treatment of inflammatory joint diseases, especially of large joints. However, short half-life of Ho is a practical impediment toward its extensive utility. This study aims to address this limitation by developing a potent formulation where Ho in transient radioactive equilibrium with Dy [T = 81.5 h] is used as its in vivo generator. In this regard, a chelator-free radiolabeling approach was optimized using porous hydroxyapatite (HA) microsphere (2-10 μm) as a carrier platform of Dy/Ho. Sorption of Dy/Ho in porous HA followed Langmuir-Freundlich isotherm and pseudo-second order kinetics, indicating chemisorption of the radiolabeling process. The formulation retained its radiochemical integrity in PBS and human serum upto a period of 14 d. The preclinical study showed near-exclusive retention of the radiolabeled microparticles within the injected joint cavity of healthy Wistar rats with no translocation of Dy and Ho. Overall, the reported studies indicated the potency developed Dy/Ho-labeled porous HA microsphere for the treatment of inflammatory joint diseases and an in vivo generator of Ho.

摘要

钬 - 166 [半衰期(T = 26.8)小时，最大能量(E (max))为(1.74)兆电子伏特（(48.7%)）和(1.85)兆电子伏特（(50.0%)）；γ能量(Eγ = 80.6)千电子伏特（(10.6%)）]是放射性滑膜切除术（RSV）中治疗炎症性关节疾病，尤其是大关节疾病最有前景的放射性核素之一。然而，钬的半衰期短是其广泛应用的一个实际障碍。本研究旨在通过开发一种有效的制剂来解决这一限制，该制剂中与镝[半衰期(T = 81.5)小时]处于瞬时放射性平衡的钬用作其体内发生器。在这方面，使用多孔羟基磷灰石（HA）微球（2 - 10微米）作为镝/钬的载体平台，优化了一种无螯合剂的放射性标记方法。多孔HA中镝/钬的吸附遵循朗缪尔 - 弗伦德利希等温线和准二级动力学，表明放射性标记过程为化学吸附。该制剂在PBS和人血清中长达14天保持其放射化学完整性。临床前研究表明，放射性标记的微粒几乎完全保留在健康Wistar大鼠注射的关节腔内，镝和钬没有发生移位。总体而言，所报道的研究表明开发的镝/钬标记的多孔HA微球可有效治疗炎症性关节疾病，并且是钬的体内发生器。

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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/badf/12092808/1a5a3b95282f/41598_2025_2373_Fig8_HTML.jpg
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