Chongqing Chemical Industry Vocational College, Chongqing 401228, China; Department of Chemistry, Tsinghua University, Beijing 100084, China.
Chongqing Chemical Industry Vocational College, Chongqing 401228, China.
Carbohydr Polym. 2020 May 15;236:116094. doi: 10.1016/j.carbpol.2020.116094. Epub 2020 Feb 29.
Different size and morphology monodispersed chitosan (CS) microspheres loaded with the anticancer drug of 5-fluorouracil (5-Fu) were prepared by the microfluidic method assisted by a crosslinking unit with crosslinkers of tripolyphosphate (TPP) and glutaraldehyde (GTA). The sizes, morphologies, drug loading, encapsulation efficiency, drug release and cytotoxicity of 5-Fu loaded CS microspheres were characterized and determined. Results indicated that the CS microspheres were uniform in size distributions. They possessed excellent encapsulation efficiency and drug loading. The TPP-crosslinked CS microspheres had rough surfaces and exhibited faster drug release, whereas the CS microspheres crosslinked with GTA had smooth surfaces and showed slower drug release. Furthermore, 5-Fu-loaded CS microspheres exhibited sustained drug release which well fitted the first-order kinetics model and were pH-responsive in that the drug cumulative release was greater at acidic environments than at neutral conditions. Finally, 5-Fu loaded CS microspheres provided sufficient cytotoxicity and were satisfactory in the cancer cell inhibition.
不同大小和形态的单分散壳聚糖（CS）微球通过微流控法制备，该方法借助带有三聚磷酸（TPP）和戊二醛（GTA）交联剂的交联单元。负载 5-氟尿嘧啶（5-Fu）的 CS 微球的大小、形态、载药量、包封率、药物释放和细胞毒性进行了表征和测定。结果表明，CS 微球粒径分布均匀。它们具有良好的包封效率和载药量。TPP 交联的 CS 微球表面粗糙，显示出更快的药物释放，而用 GTA 交联的 CS 微球表面光滑，显示出较慢的药物释放。此外，负载 5-Fu 的 CS 微球表现出持续的药物释放，符合一级动力学模型，并且具有 pH 响应性，即在酸性环境下药物累积释放大于中性条件下。最后，负载 5-Fu 的 CS 微球提供了足够的细胞毒性，对癌细胞的抑制作用令人满意。
