硫酸庆大霉素-壳聚糖纳米粒的制备及性能评价

背景：庆大霉素珠链是较早用于治疗慢性骨髓炎的局部释药系统,但是由于其不能在体内降解吸收,须二次取出,因而限制了其的应用。因此国内外学者一直致力于可吸收材料负载抗生素装置的研究。目的：制备负载庆大霉素的壳聚糖纳米粒,评价其性能,观察其体外释药行为及体外抗金黄色葡萄球菌的作用。方法：以壳聚糖为药用载体,硫酸庆大霉素为模型药物,三聚磷酸钠为离子交联剂,采用离子交联法制备庆大霉素-壳聚糖纳米粒,在MH平板上进行抑菌实验,观察及评价其抑制金黄色葡萄球菌的作用。结果与结论：制备的纳米粒形态为类圆形,粒径为40~70 nm,包封率及载药量分别为31.3%和15.4%,体外释药可持续14 d左右,对金黄色葡萄球菌的体外抑菌效果可持续25 d,在第5天纳米粒的抑菌作用达到最大,随着时间的推移,抑菌圈逐渐缩小。

Preparation and characteristics of gentamicin sulfate-loaded chitosan nanospheres

BACKGROUND: Gentamicin beads as a local drug delivery system was earlier used for the treatment of chronic osteomyelitis of the local drug delivery system, but due to its degradation and absorption in the body, it cannot be the second out, thus its application is limited. Therefore, domestic and foreign scholars have been working to study absorbable materials loaded with antibiotics device.OBJECTIVE: To formulate the gentamicin sulfate-loaded chitosan nanospheres (GS-CS nanospheres) and to evaluate its performance and to study its releasing behavior and the anti-staph aureus efficacy in vitro.METHODS: The GS-CS nanospheres were prepared by ion cross-linking technique using chitosan as drug carrier and gentamicin sulfate as model drug and sodium tripolyphosphate as crosslinker reagent. The drug loading and encapsulation efficiency were estimated. The releasing behavior of the GS-CS nanospheres was studied and the diameter of inhibition zone of the GS-CS nanospheres was measured.RESULTS AND CONCLUSION: The nanospheres were spherical with the diameter ranging from 40 nm to 70 nm, the encapsulation efficiency and drug loading were estimated to be 31.3% and 15.4%, respectively. In vitro releasing behavior could continue about 14 days; the anti-staph aureus efficacy in vitro could continue about 25 days, the greatest anti-staph aureus efficacy reached at 5 days and then decreased gradually.