卡铂碳包铁纳米笼壳聚糖纳米球的制备和特征  

Preparation and Characteristics of Carboplatin-Fe@C Nanocage-Loaded Chitosan Nanoparticles

作　　者：郭跃华[1] 李富荣 韩涛[3] 桂玲[4] 鲍世韵[1] 周汉新 

机构地区：[1]华中科技大学同济医学院附属协和医院肝胆外科,武汉430022 [2]暨南大学第二临床医学院深圳市人民医院临床医学研究中心,广东深圳518020 [3]暨南大学化学院,广州510632 [4]华中科技大学同济医学院药理系,武汉430022

出　　处：《中国药学杂志》2007年第1期43-47,共5页Chinese Pharmaceutical Journal

基　　金：广东省自然科学基金资助项目(04006966);广东省名医工程研究项目;深圳市科技计划项目(2002-K3-121)

摘　　要：目的制备双重物理机制载药的卡铂碳包铁纳米笼壳聚糖纳米球,优选制备工艺,观测其特征。方法碳包铁纳米磁粉经稀盐酸处理后制得碳包铁纳米笼。以此纳米笼为磁性内核,壳聚糖为基质,采用反相微乳法制备卡铂碳包铁纳米笼壳聚糖纳米球。该纳米球通过基质包裹和碳包铁纳米笼吸附双重物理机制载药。利用正交实验设计优选纳米球制备工艺,观测纳米球的形貌、粒径、载药量、磁响应性和体外释药性能。结果碳包铁纳米笼与其前体相比,比表面积由20.98 m2.g-1增至40.38 m2.g-1,孔容由70 mm3.g-1增至110mm3.g-1,对卡铂的吸附量为9.6%。卡铂碳包铁纳米笼壳聚糖纳米球球形圆整,磁响应性强,平均粒径(207±21)nm,载药量为(11.40±1.31)%。纳米球的体外释药持续5 d,累计释药量依次为51%,68%,80%,87%,91%。结论良好的磁性内核和双重物理载药机制的有机结合能够优化纳米球的性能,制备出理想的磁靶向纳米药物载体。OBJECTIVE To prepare the carboplatin-Fe@ C nanocage-loaded chitosan nanoparticles using dual physical drug-loaded mechanisms,optimize the conditions of preparation and observe its characteristics. MIETHODS The Fe@ C nanocage was made from the Fe@ C nanopowder using the diluted HCl. The carboplatin-Fe@ C nanocage-loaded chitosan nanoparticles was prepared by the reverse microemulsion method. The prepared nanoparticles consisted of Fe@ C nanocage as magnetic core and chitosan as matrix. The carboplatin was loaded into the nanoparticles through dual physical mechanisms such as the encapsulation of matrix and the adsorption of Fe@ C nanocage. The orthogonal experimental design was applied to optimize the preparation procedure. The shape, size, drug content, magnetic responsivity and drug release in vitro were determined. RESULTS Compared with Fe@ C nanopowder, the specific surface area of Fe@ C nanocage increased from 20. 98 m^2 · g^-1 to 40. 38 m^2· g^-1 ,the pore volume of Fe@ C nanocage increased from 70 mm^3 · g^-1 to 110 mm^3 · g^ -1, and the content of absorption for carboplatin reached 9.6%. The carboplatin-Fe@ C nanocage-loaded chitosan nanoparticles exibited fairly smooth and spherical in shape and good magnetic responsivity. The average size was （207 ± 21 ） nm with narrow distribution. The drug content was （ 11.40 ± 1.31 ）%. The drug release in vitro lasted 5 d, and the cumulative release percents were 51% ,68% ,80% ,87% and 91%, respectively. CONCLUSION The favorable magnetic core and the rational cooperation of dual physical drug-loaded mechanisms can improve the performance of nanoparticles, and the ideal magnetic drug-loaded nano-particles can be prepared.

关 键 词：物理机制 纳米笼 磁靶向 纳米球 卡铂 壳聚糖 

分 类 号：R943[医药卫生—药剂学] R979.1[医药卫生—药学]