卡铂碳包铁纳米壳聚糖微球的制备和特征

Preparation and characteristics of carboplatin-Fe@C-loaded chitosan nanoparticles with dual physically loading-drug mechanisms

目的 制备卡铂碳包铁纳米壳聚糖微球，检测其性能，并与卡铂纯铁纳米壳聚糖微球进行比较。方法 以吸附药物的碳包铁纳米磁粉为磁性内核，壳聚糖为基质，卡铂为负载药物，采用反相微乳法制备卡铂碳包铁纳米壳聚糖微球。卡铂纯铁纳米壳聚糖微球的制备方法相似，不同的是以无吸附药物能力的纯铁纳米磁粉为磁性内核。检测和比较两种纳米药物微球的形态、粒径、磁响应性、载药量、包封率和体外释药。结果 两种药物微球的球形圆整，平均粒径（210±26）nm，粒径分布150-300nm，磁响应性强。碳包铁纳米微球的载药量（11．15±1．03）％，纯铁纳米微球载药量（9．21±1．10）％。碳包铁纳米微球1，2，3，4d的体外释药量分别为60％、74％、84％、92％；纯铁纳米微球1，2d的释药量分别为81％，91％。结论 通过活性碳吸附和物理基质包裹双重物理机制载药载药的卡铂碳包铁纳米壳聚糖微球不但载药量高，而且释药速度平稳。多重机制的有机结合是优化纳米微球性能的有效方法。

OBJECTIVE The aim of the present work was to set up the optimal carboplatin-Fe@ C-loaded chitesan nanoparticles method, compare and assess the carboplatin-Fe@ C-loaded with the carboplatin-Fe-loaded chitesan nanoperticles. METHODS The carboplatin-Fe@ C-loaded chitesan nanoparticles was prepared by reverse microemulsion method. The prepared nanoperticles consisted of Fe@ C nanopewder absorbed with drug as magnetic core, chitesan as matrix and carboplatin as model drug. The preparation of the carboplatin-Fe-loaded chitesan nanoparticles was similar. It was the difference that pure iron nanopowder which is unable to adsorb drug replaced of Fe@ C nanopewder as the core. The shape, size, magnetic respensivity, drug content, encapsulation efficiency and drug release in vitro of the two kinds of nanoparticles were determined and compared. RESULTS The two kinds of nanoparticles cxibited fairly smooth and spherical in shape with average size of 210nm±26nm （size range of 150nm-300nm） and good magnetic respensivity. The drag content of carboplafin-Fe@ C-loaded chitesan nanoparticles reached （ 11.15±1.03）%, that of carboplafin-Fe-loaded chitesan nanoparticles （9.21± 1.10） %. The cumulative release percent of the carboplatin-Fe@ C-loaded chitesan nanoparticles in vitro in 1d, 2d, 3d, 4d were 60%, 74%, 84%, 92%, respectively. On the contrast, these of oarboplatin-Fe-loaded chitesan nanoperticles in ld, 2d were 81%, 91%. CONCLUSION The carboplatin-Fe@ C-loaded chitosan nanoparticles with dual physical drugloaded mechanisms （physical encapsulation and adsorption of active carbon） possessed higher drug content and more sustained drug releasing. Thus, the cooperation of multi-mechanisms was a promising orientation to improve the properties of nanoperticles.