a Chemical and Pharmaceutical Engineering Institute , Hebei University of Science and Technology , Hebei , China.
b Tianjin Branch of Suzhou Institute of Biomedical Engineering and Technology, CAS , Tianjin , PR China.
J Microencapsul. 2019 Jan;36(1):21-31. doi: 10.1080/02652048.2019.1582723. Epub 2019 Mar 18.
The purpose of this study was to investigate the influences of drying methods on the risperidone (RIS) release profiles of RIS-loaded PLGA microspheres. These microspheres were fabricated with an O/W emulsion solvent evaporation method. The wet microspheres were dried with freeze drying and vacuum drying methods. The microspheres were mono-dispersed spheres with an average diameter of 100 μm. Studies found that drying methods had great influence on the porosity, morphology, and release profiles of RIS-loaded PLGA microspheres. Specifically, the freeze-dried microspheres had higher porosity (78.46 ± 1.64%) than those vacuum-dried ones (52.45 ± 2.68%), and they showed higher RIS release rates ( < 0.05). In the accelerated release tests (45 °C), these microspheres dried under the pressures of 700 mmHg and 200 mmHg gave faster release rates than those ones dried under the pressure of 450 mmHg. Importantly, the accelerated release test (45 °C) had a high correlation with the real-time test (37 °C) ( > 0.99). These studies exhibited a significance in the precise preparation of RIS-loaded PLGA microspheres.
本研究旨在探讨干燥方法对载利培酮(RIS)聚乳酸-乙醇酸共聚物(PLGA)微球释放曲线的影响。这些微球采用 O/W 乳液溶剂蒸发法制备。湿微球采用冷冻干燥和真空干燥方法进行干燥。微球呈单分散的球体,平均直径为 100μm。研究发现,干燥方法对载 RIS-PLGA 微球的孔隙率、形态和释放曲线有很大影响。具体来说,冷冻干燥微球的孔隙率(78.46±1.64%)高于真空干燥微球(52.45±2.68%),且它们表现出更高的 RIS 释放速率( < 0.05)。在加速释放试验(45°C)中,在 700mmHg 和 200mmHg 压力下干燥的微球比在 450mmHg 压力下干燥的微球具有更快的释放速率。重要的是,加速释放试验(45°C)与实时试验(37°C)具有高度相关性( > 0.99)。这些研究对于精确制备载 RIS-PLGA 微球具有重要意义。