Abstract：
Non-degradable, slightly degradable, and completely degradable micro/nanoparticles derived from chondroitin sulfate (CS) were synthesized through crosslinking reactions at 50%, 40%, and 20% mole ratios, respectively. The CS particles with a 20% crosslinking ratio show total degradation within 48 h, whereas 50% CS particles were highly stable for up to 240 h with only 7.0 ± 2.8% weight loss in physiological conditions (pH 7.4, 37 °C). Tobramycin and amikacin antibiotics were encapsulated into non-degradable CS particles with high loading at 250 g/mg for the treatment of corneal bacterial ulcers. The highest release capacity of 92 ± 2% was obtained for CS-Amikacin particles with sustainable and long-term release profiles. The antibacterial effects of CS particles loaded with 2.5 mg of antibiotic continued to render a prolonged release time of 240 h with 24 ± 2 mm inhibition zones against Pseudomonas aeruginosa. Furthermore, as a carrier, CS particles significantly improved the compatibility of the antibiotics even at high particle concentrations of 1000 g/mL with a minimum of 71 ± 7% fibroblast cell viability. In summary, the sustainable delivery of antibiotics and long-term treatment of bacterial keratitis were shown to be afforded by the design of tunable degradation ability of CS particles with improved biocompatibility for the encapsulated drugs.
摘要：
不可降解,轻微降解，和完全可降解的微/纳米颗粒衍生自硫酸软骨素（CS）通过交联反应在50％合成，40%,和20%的摩尔比，分别。交联率为20%的CS颗粒在48h内表现出完全降解,而50％CS颗粒在生理条件（pH7.4，37°C）下长达240小时，仅失重7.0±2.8％。妥布霉素和阿米卡星抗生素被包封在不可降解的CS颗粒中，高负载为250g/mg，用于治疗角膜细菌性溃疡。CS-阿米卡星颗粒具有可持续和长期释放的最高释放能力，为92±2％。负载有2.5mg抗生素的CS颗粒的抗菌作用继续使针对铜绿假单胞菌的24±2mm抑制区延长了240小时的释放时间。此外，作为一个载体,即使在1000g/mL的高颗粒浓度下,CS颗粒也显著改善了抗生素的相容性,其中成纤维细胞活力最低为71±7%。总之,通过设计具有可调节的降解能力的CS颗粒，并改善了封装药物的生物相容性，可以实现抗生素的可持续递送和细菌性角膜炎的长期治疗。
