反相微乳液法制备5-Fu磁性靶向药物及其释药性能

Preparation of 5-Fu Magnetic Targeting Drug in Inverse Microemulsion and study of Its Drug Release property

以5-氟脲嘧啶(5-Fu)为模型药,壳聚糖(CS)为包覆材料,纳米四氧化三铁(Fe3O4)作为磁核,戊二醛为交联剂,通过反相微乳液制备5-Fu磁性靶向纳米微粒。最佳实验条件为:乳化剂用量为8%(v/v),壳聚糖浓度为1.5%(w/w),Fe3O4/CS为0.6(w/w),复合乳化剂的HLB值为6,5-Fu/CS为0.4(w/w),油水体积比为3:1,反应温度为55℃。磁性靶向药物的产率为83.06%、载药率为13.90%、包封率达到56.67%。通过模拟胃液(pH=1.8)和肠液(pH=7.6)做体外药物缓释实验。结果显示,在两种介质中,27小时内药物释放累积释药量分别为11.90%和10.23%,一定程度上达到了缓释、延长药效的目的。

Magnetic targeting drugs were prepared by using 5-fluorouracil （5-Fu） as model drug, Fe3 04 nanoparti-eles as magnetic nucleus, chitosan （CS） as enveloping material and glutaraldehyde as cross-linking agent through inverse microemulsion technique. The optimum conditions of synthesis are surfactant 8% （v/v）, concentration of CS 1.5 % （ w/v）, Fe3 tiCS O. 6, HLB 6,5-Fu/CS 0.4, volum ratio of oil/water 3 ： 1, reacting temperature 55 ~C o The yield,drug loading and entrapment efficiency of magnetic targeting drug is 83.06% ,13.9% and 56.67% ,respec- tively. The cumulative release percent in the buffer solutions （ pH being of 1.8 and 7.6） are 11.90% and 10.23% in 27h ,respectively. The magnetic targeting drug could be released slowly and prolonged drug efficiently.