Sun S-W, Jeong Y-I, Jung S-W, Kim S-H
College of Pharmacy, Chosun University, 375, Seosuk-Dong, Dong-Gu, Kwangju 501-759, Korea.
J Microencapsul. 2003 Jul-Aug;20(4):479-88. doi: 10.1080/0265204031000093014.
In this study, the fluorescein isothiocyanate (FITC)-albumin distribution, the amount of FITC-albumin release and the degradation of poly (DL-lactic-co-glycolic acid) (PLGA) microspheres were evaluated. The higher the FITC-albumin concentration in the W1 phase, the higher the protein concentration and loading efficiency in the microspheres, the larger the particle size of microspheres. Confocal laser scanning microscopy (CLSM) showed that the FITC-albumin was distributed uniformly in the microspheres with a low concentration while it was aggregated at higher concentrations. The high protein concentration in the microspheres showed significantly large initial release (above 70% w/w) during the 10 days. A higher PVA concentration in the W2 phase resulted in a smaller particle size, higher protein contents and loading efficiency and decreased release rate. After a 10 day incubation period, the microspheres with a low FITC-albumin concentration had an almost spherical morphology, while microspheres with a high FITC-albumin concentration had a more distorted morphology, suggesting that rapid morphological changes and microspheres ruptures can be induced by an initial burst release.
在本研究中,评估了异硫氰酸荧光素(FITC)-白蛋白的分布、FITC-白蛋白的释放量以及聚(DL-乳酸-乙醇酸)(PLGA)微球的降解情况。W1相中FITC-白蛋白浓度越高,微球中的蛋白质浓度和载药效率越高,微球的粒径越大。共聚焦激光扫描显微镜(CLSM)显示,低浓度时FITC-白蛋白在微球中均匀分布,而在高浓度时则聚集。微球中高蛋白浓度在10天内显示出显著的大量初始释放(超过70% w/w)。W2相中较高的聚乙烯醇(PVA)浓度导致粒径较小、蛋白质含量和载药效率较高以及释放速率降低。经过10天的孵育期后,低FITC-白蛋白浓度的微球具有几乎球形的形态,而高FITC-白蛋白浓度的微球具有更扭曲的形态,这表明初始爆发释放可诱导快速的形态变化和微球破裂。