姜黄素纳米给药系统抗耐甲氧西林金黄色葡萄球菌的活性研究

Study on the Anti-Methicillin Resistant Staphylococcus aureus by Curcumin Nanometer Dosing System

摘要: 耐甲氧西林金黄色葡萄球菌因其极强的传染性已经成为引起院内感染的重要致病菌之一，首选药物万古霉素近年来不断出现耐药株，这使得MRSA的治疗更加棘手。姜黄素是一种天然来源的抗菌药，在抗耐药性方面有无法比拟的优点。但是姜黄素由于性质不稳定，在水中溶解性差，生物利用度低等缺点限制其临床应用。纳米粒载体能够显著提高姜黄素的水溶性和生物利用度，延长药物在体内的滞留时间并降低药物的毒副作用。本课题通过开环聚合的方法制备PET-CL高聚物为载体材料，采用溶剂挥发法制备姜黄素纳米粒，并对姜黄素纳米粒粒径，PDI，包封率和载药量进行表征。姜黄素PET-CL纳米粒稳定，其体外释放表现出明显缓释特性。此外，姜黄素PET-Cl纳米粒还具有持续的抑菌作用。上述结果可为扩大姜黄素药用范围，丰富其治疗途径和对抗菌活性机制的深入研究提供理论依据。

Abstract: MRSA (methicillin-resistant Staphylococcus aureus) has become one of the major sources of hospital-acquired infections due to the powerful infectivity. Vancomycin, the preferred drug, has been overused, inducing that the vancomycin resistant strains were constantly discovered in recent years, which made the MRSA treatment more difficult. Curcumin (Cur), a natural antiseptic, displays prominent advantages in fighting against antibiotic resistance. However, its broad clinical applicability and effectiveness are limited by aqueous insolubility, low systemic bioavailability, and instability. Nanoparticles (NPs) are efficient carriers to improve the aqueous solubility, bioavailability, the drug circulation time in the blood, and the risk of side effects of curcumin. In this work, we synthesized amphiphilic copolymers (PET-Cl) by ring-opening polymerization; NPs were then prepared via emulsion-solvent evaporation method. Meanwhile, particle size, Zeta potential, entrapment efficiency (EE) and drug-loading (DL) content of Cur nanoparticles were measured. In in vitro release study, Cur PET-Cl nanoparticles were stable, and it showed obvious sustained release characteristics in vitro. In addition, Cur PET-Cl nanoparticles displayed a persistent bacteriostatic effect. These results indicate that the study on Cur PET-Cl nanoparticles can provide theoretical basis for expanding medicinal range, enriching the therapeutic pathway and improving the antibacterial activity mechanism research.