Chitosan and β-cyclodextrin Microspheres as Pulmonary Sustained Delivery Systems  

作　　者：ZHANG Weifen CHEN Xiguang LI Piwu HE Qiangzhi ZHOU Huiyun CHA Dongsu 

机构地区：[1]College of Marine Life Science, Ocean University of China, Qingdao 266003, China [2]Shandong Academy of Food and Fermentation Industries, Jinan 250013, China [3]Graduate School of Biotechnology, Korea University, Seoul 136-701, Korea [4]Depantment of Pharmacy, Weifang Medical University, Weifang 261042, China

出　　处：《Journal of Wuhan University of Technology(Materials Science)》2008年第4期541-546,共6页武汉理工大学学报（材料科学英文版）

基　　金：the National Natural Science Foundation of China(No.30670566);Natural Science Foundation of Shandong Province

摘　　要：Chitosan and β-cyclodextrin were used to prepare microspheres with theophylline for pulmonary delivery by spray drying method. The characteristics, mucociliotoxicity, permeation rate and drug release were studied. The drug entrapments of microspheres Ⅰ, Ⅱ and Ⅲ were from 35.70% to 21.09% and 13.33%, while yields and encapsulation efficiencies were higher than 45% and about 90% respectively. The microspheres possessed low tap densities （0.34-0.48 g/cm^3）, appropriate diameters （3.35-3.94 μm） and theoretical aerodynamics diameters （2.20-3.04 μm）. SEM images showed the microspheres were spherical with smooth or wrinkled surface surfaces. FT-IR demonstrated theophylline had formed hydrogen bonds with chitosan and fl-cyclodextrin. The microspheres could effectively reduce the ciliotoxicity and easy to penetrate the memberine. The in vitro release of the microspheres was related to the ratio of drug/polymer and microspheres Ⅱ had a prolong release, providing the release of 72.00% in 12 h. The results suggestes that chitosan/β-cyclodextrin microspheres Ⅱ are a promising carrier as sustained release for pulmonary delivery.Chitosan and β-cyclodextrin were used to prepare microspheres with theophylline for pulmonary delivery by spray drying method. The characteristics, mucociliotoxicity, permeation rate and drug release were studied. The drug entrapments of microspheres Ⅰ, Ⅱ and Ⅲ were from 35.70% to 21.09% and 13.33%, while yields and encapsulation efficiencies were higher than 45% and about 90% respectively. The microspheres possessed low tap densities （0.34-0.48 g/cm^3）, appropriate diameters （3.35-3.94 μm） and theoretical aerodynamics diameters （2.20-3.04 μm）. SEM images showed the microspheres were spherical with smooth or wrinkled surface surfaces. FT-IR demonstrated theophylline had formed hydrogen bonds with chitosan and fl-cyclodextrin. The microspheres could effectively reduce the ciliotoxicity and easy to penetrate the memberine. The in vitro release of the microspheres was related to the ratio of drug/polymer and microspheres Ⅱ had a prolong release, providing the release of 72.00% in 12 h. The results suggestes that chitosan/β-cyclodextrin microspheres Ⅱ are a promising carrier as sustained release for pulmonary delivery.

关 键 词：THEOPHYLLINE CHITOSAN SPRAY-DRYING MICROSPHERES pulmonary delivery 

分 类 号：O636[理学—高分子化学]