Biodegradable micro- and nanoparticles as long-term delivery vehicles for gentamicin
Biodegradable micro- and nanoparticles as long-term delivery vehicles for gentamicin
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DOI：
10.1080/02652040600946886
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发表时间：
2006-11-01
影响因子：
3.9
通讯作者：
Blanco-Prieto, Maria J.
中科院分区：
文献类型：
--
作者：
Lecaroz, Concepcion;Gamazo, Carlos;Blanco-Prieto, Maria J.
采用溶剂挥发法制备了庆大霉素的聚乳酸-羟基乙酸共聚物（PLGA）微球和纳米球，目的是获得合适的全身给药载体。微球的平均直径小于3 mm，纳米颗粒显示出均匀的尺寸，直径为320 nm。在微囊化的情况下，药物负载更有效。具有羧基端基的更亲水的共聚物产生更高的微粒负载，达到高达9.2 μ g mg（-1）的聚合物（502 H、503 H或75：25 H）的包封效率。由502 H PLGA制成的纳米颗粒也达到了可接受的包封水平（6.2 μ g（-1））。通过使用溶剂蒸发方法制备的颗粒显示水合后没有聚集，与通过喷雾干燥制备的微粒形成对比，所述微粒显示快速且高的自动聚集。体外释放曲线显示，503 H微球在第一个小时内表现出最高的突释，而最持续的释放是502 H共聚物的微粒（28天后40%的庆大霉素保留在制剂中）。总之，由502 H、503 H和75：25 H制成的微球和502 H的纳米颗粒显示出用于治疗细胞内庆大霉素敏感病原体的全身使用的最佳潜在性质。
Micro-and nanoparticles of poly(lactide-co-glycolide)( PLGA) loading gentamicin were prepared by a solvent evaporation method with the aim of obtaining appropriate vectors for systemic administration. Microspheres presented mean diameters below 3 mm and nanoparticles showed homogeneous sizes with a diameter of 320 nm. Drug loading was more efficient in the case of microencapsulation. The more hydrophilic copolymers with carboxyl-end groups yielded higher microparticle loadings, reaching encapsulation efficiencies up to 9.2 mu g mg(-1) of polymer (502H, 503H or 75:25H). Nanoparticles made of 502H PLGA also achieved an acceptable level of encapsulation (6.2 mu gmg(-1)). Particles prepared by using the solvent evaporation method showed no aggregation after hydration, in contrast to the microparticles prepared by spray-drying which showed fast and high auto-aggregation. In vitro release profiles revealed that 503H microspheres showed the highest burst during the first hour, while the most sustained release was for microparticles of 502H copolymer (40% of gentamicin remained in the formulation after 28 days). In summary, microspheres made of 502H, 503H and 75:25H and nanoparticles of 502H showed the best potential properties for systemic use in the treatment of intra-cellular gentamicin-susceptible pathogens.