一种负载分选酶A抑制剂的聚甲基丙烯酸甲酯骨水泥的配方与表征

Formulation and characterization of a sortase a inhibitor-loaded PMMA bone cement.

作者信息

Qi Yin-Yu, Han Lu-Yang, Han Long-Xu, Bu Wen-Han, Xu Yang, Chu Jian-Jun

机构信息

Bengbu Medical University, The Second People's Hospital of Hefei (Affiliated Hospital) Anhui 230011 China

Department of Pharmaceutical Science and Engineering, Hefei University of Technology Hefei Anhui 230009 China.

出版信息

RSC Adv. 2025 Sep 17;15(41):33966-33975. doi: 10.1039/d5ra04437e.

DOI:10.1039/d5ra04437e

PMID:40969824

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12442756/

Abstract

A sortase A inhibitor (SrtA I)-loaded bone cement (SLBC) containing 1-(3,4-dichlorophenyl)-3-(dimethylamino)propyl-1-one hydrochloride (AEEK1) was reported. Compared with gentamicin-loaded bone cement (GS cement), which is a widely used antibiotic-loaded bone cement in cemented total joint replacement (TJR), SLBC demonstrated a significantly prolonged effective antibacterial duration against both () and methicillin-resistant (MRSA). The quasi-static compressive strength, maximum polymerization temperature, and setting time of SLBC were within the limits stated in the ISO 5833 standard and comparable to the corresponding values of GS cement. and experimental results confirmed the biocompatibility of SLBC and showed its easy injectability into porcine T12 vertebrae. Taken together, these findings suggest that SLBC may have potential for managing/treating prosthetic joint infections, which is a common complication in cemented TJR.

摘要

据报道，有一种载有分选酶A抑制剂（SrtA I）的骨水泥（SLBC），其含有1-(3,4-二氯苯基)-3-(二甲基氨基)丙基-1-酮盐酸盐（AEEK1）。与庆大霉素载药骨水泥（GS骨水泥）相比，后者是在骨水泥型全关节置换术（TJR）中广泛使用的载抗生素骨水泥，SLBC对金黄色葡萄球菌（）和耐甲氧西林金黄色葡萄球菌（MRSA）均表现出显著延长的有效抗菌持续时间。SLBC的准静态抗压强度、最高聚合温度和凝固时间均在ISO 5833标准规定的范围内，且与GS骨水泥的相应值相当。体内和体外实验结果证实了SLBC的生物相容性，并表明其易于注入猪的T12椎体。综上所述，这些发现表明SLBC在处理/治疗人工关节感染方面可能具有潜力，人工关节感染是骨水泥型TJR中的常见并发症。