Kusonwiriyawong Chirasak, Pichayakorn Wiwat, Lipipun Vimolmas, Ritthidej Garnpimol C
Faculty of Pharmaceutical Sciences, Department of Manufacturing Pharmacy, Chulalongkorn University, Bangkok, Thailand.
J Microencapsul. 2009 Mar;26(2):111-21. doi: 10.1080/02652040802190937.
Chitosan microparticles for delivery of proteins were prepared by spray-drying technique. The effects of formulation (molecular weight and concentration of chitosan) and process variables (inlet drying air temperature and spray rate) on size and morphology of microparticles were characterized. Size of microparticles was mainly controlled by formulation variables, while particle morphology was influenced by both formulation and process variables investigated in this study. Bovine serum albumin (BSA), as a model protein, was loaded into microparticles at different levels. BSA-loaded chitosan microparticles were characterized in terms of physicochemical properties and integrity of encapsulated protein, which was studied by sodium dodecyl sulphate-polyacrylamide gel electrophoresis and circular dichroism. Size of microparticles ranged between 3.760-8.681 microm, of which BSA-loaded microparticles were larger in size than their corresponding blank microparticles. All microparticles showed dented or distorted surface, especially when BSA was incorporated, with positive surface charge exposed. Burst release of protein was observed. The effect was more pronounced as BSA loading level was increased. Integrity of entrapped protein could be retained when BSA was incorporated at high loading level. In conclusion, chitosan microparticles for delivery of protein could be efficiently prepared by spray-drying technique. The encapsulated protein was capable of retaining its integrity after the preparation process.
采用喷雾干燥技术制备了用于蛋白质递送的壳聚糖微粒。研究了配方（壳聚糖的分子量和浓度）和工艺变量（进风干燥温度和喷雾速率）对微粒尺寸和形态的影响。微粒尺寸主要受配方变量控制，而颗粒形态受本研究中考察的配方和工艺变量的共同影响。以牛血清白蛋白（BSA）作为模型蛋白，将其以不同水平载入微粒中。对载有BSA的壳聚糖微粒的理化性质和包封蛋白的完整性进行了表征，通过十二烷基硫酸钠-聚丙烯酰胺凝胶电泳和圆二色性对其进行了研究。微粒尺寸在3.760 - 8.681微米之间，其中载有BSA的微粒尺寸大于相应的空白微粒。所有微粒均呈现凹陷或扭曲的表面，尤其是当加入BSA时，表面带有正电荷。观察到蛋白质的突释现象。随着BSA载入水平的提高，这种效应更为明显。当以高载入水平加入BSA时，包封蛋白的完整性能够得以保留。总之，采用喷雾干燥技术能够有效地制备用于蛋白质递送的壳聚糖微粒。制备过程后，包封的蛋白能够保持其完整性。
