叶酸偶联5-氟尿嘧啶壳聚糖纳米粒的制备及其体外性质研究

Preparation of folate-conjugated 5-fluorouracil-chitosan nanoparticles and its property evaluation in vitro

目的研究叶酸偶联壳聚糖载5-氟尿嘧啶纳米粒的制备方法及体外性质。方法根据叶酸与壳聚糖的偶联比选择最佳工艺条件,通过叶酸活性酯与壳聚糖上的氨基反应,制备叶酸偶联壳聚糖,再通过离子交联法制备叶酸偶联壳聚糖纳米粒包合5-氟尿嘧啶,从而制成载药纳米粒。结果制备了叶酸壳聚糖偶联物,并包合5-氟尿嘧啶成纳米粒,载药量为10.4%,包封率为50.5%,8 h累积释药量达35.9%。结论优化了叶酸偶联5-氟尿嘧啶壳聚糖纳米粒的制备工艺。

Objective To prepare folate-conjugated 5-fluorouracil-chitosan nanoparticles（5-FU-CSNP-folate） and evaluate its property in vitro.Methods The optimal technological conditions were selected according to the conjugated ratio of folate and chitosan.Folate-conjugated chitosan was prepared by the reaction of the activated folate ester with the amine group of chitosan.Folate-conjugated 5-fluorouracil-chitosan nanoparticles were then prepared with ionic cross-linking.Results Folate-conjugated 5-fluorouracil-loaded chitosan was prepared through different ways,and nanoparticles loading 5-FU was prepared.The encapsulation ratio of 5-FU-CSNP-folate was 50.5% and the drug loading was 10.4%.The total amount of accumulated release was 35.9% at the eighth hour.Conclusions The preparation condition of 5-FU-CSNP-folate was optimized.