Chen C Q, Lin W, Coombes A G, Davis S S, Illum L
Department of Pharmaceutical Sciences, University of Nottingham, University Park, UK.
J Microencapsul. 1994 Jul-Aug;11(4):395-407. doi: 10.3109/02652049409034257.
Human serum albumin (HSA) microspheres have been produced in the size range of 200 nm to 10 microns by the controlled addition of acetone to an aqueous solution of HSA, followed by stabilization of the formed microspheres at an elevated temperature. Microspheres produced by this acetone-heat denaturation method could be stabilized at relatively low temperatures (75 degrees C) over a short time period (15-30 min). The acetone-heat denaturation method is different from the traditional oil/water technique for preparation of HSA microspheres, both in terms of production method and the avoidance of high temperatures (> 100 degrees C) and extended heating times (> 30 min) for stabilization. This paper describes the influence of process conditions, such as volumes of acetone and HSA concentration, on the formation of the microspheres and their morphological characteristics. A loading efficiency of 8 per cent was achieved for the HSA microspheres when using rose bengal as a model compound. The release of rose bengal from the microspheres in phosphate buffered saline at 37 degrees C was dependent on the presence of the surfactant Tween 80, and varied from a 5 per cent release in 14 days in the absence of surfactant to a 50 per cent release in 8 h in the presence of surfactant.
通过向人血清白蛋白（HSA）水溶液中控制性地添加丙酮，随后在升高的温度下稳定所形成的微球，已制备出尺寸范围在200纳米至10微米的人血清白蛋白微球。通过这种丙酮 - 热变性方法制备的微球可在相对较低的温度（75摄氏度）下在短时间内（15 - 30分钟）实现稳定化。丙酮 - 热变性方法在生产方法以及避免高温（>100摄氏度）和延长稳定化所需的加热时间（>30分钟）方面，与传统的油/水技术制备HSA微球不同。本文描述了诸如丙酮体积和HSA浓度等工艺条件对微球形成及其形态特征的影响。当使用孟加拉玫瑰红作为模型化合物时，HSA微球的负载效率达到了8%。在37摄氏度的磷酸盐缓冲盐水中，孟加拉玫瑰红从微球中的释放取决于表面活性剂吐温80的存在，在不存在表面活性剂的情况下，14天内释放率为5%，而在存在表面活性剂的情况下，8小时内释放率为50%。
