Novel sustained release microspheres for pulmonary drug delivery
Novel sustained release microspheres for pulmonary drug delivery
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DOI：
10.1016/j.jconrel.2005.01.003
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发表时间：
2005-05-05
影响因子：
10.8
通讯作者：
Kellaway, IW
中科院分区：
文献类型：
--
作者：
Cook, RO;Pannu, RK;Kellaway, IW
描述了一种产生用于肺部给药的缓释(SR)颗粒的新方法。使用喷雾干燥方法将亲水性、离子化药物的高纯度纳米颗粒包裹在疏水微球中。模型药物特布他林(TS)从微球中的缓释与载药量和磷脂含量成正比。载药量为33%的微球在磷酸盐缓冲液中180min的缓释率为32.7%。在模拟肺液中的释放没有显著差异。在喷雾干燥过程中，没有观察到明显的突释现象，这表明纳米颗粒被有效地包覆。共聚焦显微镜证实微球表面没有纳米颗粒。缓释微球作为无载体干粉用于吸入，表现出46.5+/-1.8%的良好细颗粒分数(FPF)和3.93+/-0.12微米的空气动力学质量中值(MMAD)。(C)2005年由Elsevier B.V.发表。
A novel process for generating sustained release (SR) particles for pulmonary drug delivery is described. High purity nanoparticles of a hydrophilic, ionised drug are entrapped within hydrophobic microspheres using a spray-drying approach. Sustained release of the mode) drug, terbutaline sulphate (TS), from the microspheres was found to be proportional to drug loading and phospholipid content. Microspheres with a 33% drug loading exhibited sustained release of 32.7% over 180 min in phosphate buffer. Release was not significantly different in simulated lung fluids. No significant burst release was observed which suggested that nanoparticles were coated effectively during spray-drying. The absence of nanoparticles at the microsphere surface was confirmed with confocal microscopy. The sustained release microspheres were formulated as a carrier-free dry powder for inhalation, and exhibited a favourable Fine Particle Fraction (FPF) of 46.5 +/- 1.8% and Mass Median Aerodynamic Diameter (MMAD) of 3.93 +/- 0.12 mu m. (c) 2005 Published by Elsevier B.V.