新型利福平缓释植入支架材料的制备及体内缓释分析

发布时间：2018-04-17 17:21

本文选题：骨结核 + 复合支架材料　；参考：《南方医科大学学报》2016年03期

【摘要】：目的制备一种可局部植入的具有良好的药物缓释以及成骨性能的新型材料并验证其缓释性能和生物安全性。方法使用乳化溶媒挥发法制备利福平-聚乳酸羟基乙酸共聚物载药微球并将其与带负电荷硫酸钙/β-磷酸三钙复合骨水泥结合制备成一种新型的复合抗结核支架材料。分别观察微球以及复合支架材料的体外缓释性能。通过在成年雄性SD大鼠的肌袋模型中植入复合抗结核支架材料来观察不同时间点的局部药物浓度以及血药浓度,通过血生化指标以及肝脏病理组织切片评价复合抗结核支架材料的体内安全性。结果利福平/聚乳酸羟基乙酸共聚物载药微球的包封率和载药率分别为(56.05±5.33)%和(29.80±2.88)%。在第28天微球和复合支架材料的体外累积释放率分别为(94.19±5.40)%和(82.23±6.28)%。局部植入抗结核复合支架材料后药物缓释效果令人满意,在术后第28天局部药物浓度仍可达到16.18±0.35μg/g。血浆生化指标提示局部植入抗结核复合支架材料后会出现一过性肝损伤,肝脏病理切片的结果显示在第28天肝损伤基本得到完全修复。结论利福平-聚乳酸羟基乙酸共聚物载药微球-带负电荷硫酸钙/β-磷酸三钙复合骨水泥作为一种新型的抗结核局部植入物,具有良好的缓释效果以及生物相容性,能弥补传统抗结核疗法局部药物浓度过低的不足。
[Abstract]:Objective to prepare a new material with good drug delivery and osteogenic properties and verify its sustained release and biological safety.Methods rifampicin-polylactic acid copolymer microspheres were prepared by emulsified solvent volatilization method and combined with negatively charged calcium sulfate / 尾 -tricalcium phosphate composite bone cement to form a new composite anti-tuberculous scaffold material.The in vitro slow release properties of microspheres and composite scaffolds were observed.The local drug concentration and blood drug concentration at different time points were observed by implanting composite anti-tuberculosis scaffold material into the muscle bag model of adult male SD rats.The in vivo safety of composite anti-tuberculosis scaffold was evaluated by blood biochemical indexes and liver pathological sections.Results the encapsulation efficiency and drug loading rate of rifampicin / polylactic acid copolymer microspheres were 56.05 卤5.33% and 29.80 卤2.88%, respectively.On the 28th day, the cumulative release rates of microspheres and composite scaffolds were 94.19 卤5.40% and 82.23 卤6.28%, respectively.After local implantation of anti-tuberculosis composite stent, the drug release was satisfactory, and the local drug concentration reached 16.18 卤0.35 渭 g / g on the 28th day after operation.The plasma biochemical indexes suggested that temporary liver injury would occur after local implantation of anti-tuberculosis composite scaffolds. The results of pathological sections of the liver showed that the liver injury was basically repaired completely on the 28th day.Conclusion Rifampicin-poly (lactic acid) glycolic acid copolymer microspheres with negative charge calcium sulfate / 尾 -tricalcium phosphate composite bone cement as a new type of anti-tuberculous local implants have good slow-release effect and biocompatibility.It can make up for the deficiency of local drug concentration of traditional anti-tuberculosis therapy.
【作者单位】：南方医科大学南方医院脊柱骨科;
【基金】：国家自然科学基金(81272022)~~
【分类号】：R318.08

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