PLIVA Croatia Ltd., Research and Development, Prilaz baruna Filipovića 29, 10000 Zagreb, Croatia.
J Microencapsul. 2011;28(2):108-21. doi: 10.3109/02652048.2010.535620.
Spray dried microparticles containing mupirocin calcium were designed as acrylic matrix carriers with modulated drug release for efficient local drug delivery at minimum daily dose. Particle generation in spray drying and its effect on release performance were assessed by varying drug : polymer ratios with consequently altered initial saturations. Narrow-sized microparticles with mean diameters of 1.7-2.5 µm were obtained. Properties of the generated solid dispersions were examined by X-ray, thermal (thermogravimetric analysis, modulated differential scanning calorimetry) and spectroscopic (Fourier transformed infrared, Fourier transformed Raman) methods and correlated with drug loading and in vitro release. The best control over mupirocin release was achieved for 2 : 1 (w/w) drug : polymer ratio and found to be strongly process-dependent. For a particular ratio, increased feed concentration (>4%) boosted while increased inlet temperature (≥ 100 °C) reduced drug release. Antimicrobial activity testing confirmed that encapsulated drug preserved its antibacterial effectiveness. Conclusively, spray drying was proven as a suitable method for preparing structured microparticles which can control drug release even at exceptionally high drug loadings.
载有莫匹罗星钙的喷雾干燥微球被设计为具有调节药物释放的丙烯酸基质载体，可在最低日剂量下实现高效局部药物递送。通过改变药物与聚合物的比例，从而改变初始饱和度，评估喷雾干燥中的颗粒生成及其对释放性能的影响。获得了平均直径为 1.7-2.5μm 的窄粒径微球。通过 X 射线、热（热重分析、调制差示扫描量热法）和光谱（傅里叶变换红外、傅里叶变换拉曼）方法检查生成的固体分散体的性质，并将其与药物负载和体外释放相关联。对于 2:1（w/w）药物与聚合物的比例，可以实现对莫匹罗星释放的最佳控制，并且发现其强烈依赖于工艺。对于特定比例，增加进料浓度（>4%）会增加药物释放，而增加入口温度（≥100°C）会降低药物释放。抗菌活性测试证实，包封的药物保持了其抗菌效果。总之，喷雾干燥被证明是一种合适的方法，可用于制备结构微球，即使在异常高的药物载量下也可以控制药物释放。
