Tsung M, Burgess D J
Department of Pharmaceutical Sciences, School of Pharmacy, University of Connecticut, Storrs 06269-2092, USA.
J Pharm Sci. 1997 May;86(5):603-7. doi: 10.1021/js9603257.
The aims of this study are to optimize conditions for the preparation, stabilization, and harvesting of heparin/gelatin microcapsules prepared by complex coacervation. Microelectrophoresis and dry coacervate weight were used to determine the optimum conditions of pH and ionic strength for maximum heparin/gelatin coacervate yield. Heparin/gelatin microcapsules were formed by complex coacervation in the presence and absence of poly(1-vinyl-2-pyrrolidone) (PVP), which was used as a stabilizer. The microcapsules were collected using a spray-drying technique. Microcapsule particle size was analyzed using an AccuSizer optical sizer. Optimized conditions for maximum coacervate yield were pH 2.6, ionic strength 10 mM, and a 1:2 heparin/gelatin A ratio. PVP stabilized the heparin/gelatin coacervate droplets and reduced droplet aggregation during spray-drying. The mean particle diameter of the spray-dried coacervate droplets was lower in the presence of PVP and was unaffected by PVP concentration (in the range 0.5-2.0% w/w). Heparin/gelatin microcapsules, prepared under conditions optimized for maximum coacervate yield, were stabilized without the use of chemical cross-linking agents. Stabilization was achieved by a combination of the addition of PVP and spray-drying.
本研究的目的是优化通过复凝聚法制备、稳定化和收获肝素/明胶微胶囊的条件。采用微电泳和干凝聚物重量法来确定pH值和离子强度的最佳条件,以实现最大的肝素/明胶凝聚物产率。在有和没有用作稳定剂的聚(1-乙烯基-2-吡咯烷酮)(PVP)存在的情况下,通过复凝聚法形成肝素/明胶微胶囊。使用喷雾干燥技术收集微胶囊。使用AccuSizer光学粒度仪分析微胶囊的粒径。实现最大凝聚物产率的优化条件为pH 2.6、离子强度10 mM以及肝素/明胶A比例为1:2。PVP稳定了肝素/明胶凝聚液滴,并减少了喷雾干燥过程中的液滴聚集。在PVP存在的情况下,喷雾干燥凝聚液滴的平均粒径较小,且不受PVP浓度(0.5 - 2.0% w/w范围)的影响。在为实现最大凝聚物产率而优化的条件下制备的肝素/明胶微胶囊,无需使用化学交联剂即可实现稳定化。通过添加PVP和喷雾干燥相结合实现了稳定化。