Luo Shang, Man Hua, Jia Xile, Li Yuanyuan, Pan Aihong, Zhang Xuecheng, Song Yimin
Colloge of Chemical Engineering, Qingdao University of Science and Technology, Qingdao, P.R. China.
Colloge of Marines Life Science, Ocean University of China, Qingdao, P.R. China.
Des Monomers Polym. 2018 Oct 16;21(1):172-181. doi: 10.1080/15685551.2018.1534317. eCollection 2018.
Chitosan (CS)-acetylsalicylic acid (ASA) nanoparticles, which are well dispersed and stable in aqueous solution, have been prepared by interpolymer complexation of ASA in CS solution. The physicochemical properties of nanoparticles were investigated by using FT-IR, H NMR, scanning electron microscope（SEM）, dynamic light scattering, and UV spectrophotometer. It was found that the carboxyl group of the ASA had firmly integrated on the amino group of CS and the ASA-CS nanoparticles were almost spherical in shape with an average diameter of less than (79.3 ± 24.6) nm in high reproducibility and showed high chemical stability against environmental changes. It was also found that the prepared nanoparticles carried a positive charge and showed the size in the range from 700 to 150 nm. The surface structure and zeta potential of nanoparticles can be controlled by different preparation processes. The factor experiment results indicated that the ASA-CS nanoparticles had satisfactory loading capacity (LC) and encapsulation efficiency (EE), 27.27% and 46.88% (data not shown), respectively. The experiments of in ASA release showed that these nanoparticles provided a sustained and pH-dependent drug release manner, and the release behavior was influenced by the pH value of the medium. Preliminary pharmacology experiment exhibited prolonged circulation and higher bioavailability than that of ASA. All the results indicated that ASA/CS nanoparticles may have promising pharmaceutical application, and further pharmacological research is needed to confirm these beneficial effects.
壳聚糖（CS）-乙酰水杨酸（ASA）纳米颗粒通过ASA在CS溶液中的聚合物间络合作用制备而成，在水溶液中分散良好且稳定。利用傅里叶变换红外光谱（FT-IR）、核磁共振氢谱（H NMR）、扫描电子显微镜（SEM）、动态光散射和紫外分光光度计对纳米颗粒的物理化学性质进行了研究。结果发现，ASA的羧基已牢固地整合在CS的氨基上，ASA-CS纳米颗粒几乎呈球形，平均直径小于（79.3±24.6）nm，重现性高，并且对环境变化具有高化学稳定性。还发现所制备的纳米颗粒带正电荷，尺寸在700至150nm范围内。纳米颗粒的表面结构和zeta电位可通过不同的制备工艺进行控制。因素实验结果表明，ASA-CS纳米颗粒具有令人满意的载药量（LC）和包封率（EE），分别为27.27%和46.88%（数据未显示）。ASA释放实验表明，这些纳米颗粒提供了一种持续且依赖pH的药物释放方式，释放行为受介质pH值的影响。初步药理学实验显示，其循环时间延长，生物利用度高于ASA。所有结果表明，ASA/CS纳米颗粒可能具有良好的药物应用前景，需要进一步的药理学研究来证实这些有益效果。
