CAJ | 학술논문

目的：制备胰岛素巯基化透明质酸纳米粒（insulin thiolated hyaluronic acid nanoparticles，Ins-HA-Cys-NPs），考察纳米粒的理化性质。方法以合成的具有生物黏附性质的巯基化透明质酸作为载体，采用超声乳化法制备纳米粒，考察其外观、粒径、Zeta电位、包封率、载药量，并进行其冻干制剂的冻干保护剂筛选。结果制备的Ins-HA-Cys-NPs粒径均一，外观圆整；平均粒径为（178.5±0.8）nm，PDI为（0.214±0.013），Zeta电位为-（38.47±0.46）mV，超滤离心法测定载药纳米粒的包封率为（48.85±0.66）％，载药量为（4.79±0.13）％；选择10％的甘露醇为冻干保护剂，复溶后得到具有蓝色乳光的粒径均一的纳米粒混悬液。结论巯基化透明质酸纳米粒是蛋白多肽类药物口服给药的潜在载体，为下一步研究胰岛素纳米粒在大鼠体内药效、药动学研究提供前提和基础。
목적：제비이도소구기화투명질산납미립（insulin thiolated hyaluronic acid nanoparticles，Ins-HA-Cys-NPs），고찰납미립적이화성질。방법이합성적구유생물점부성질적구기화투명질산작위재체，채용초성유화법제비납미립，고찰기외관、립경、Zeta전위、포봉솔、재약량，병진행기동간제제적동간보호제사선。결과제비적Ins-HA-Cys-NPs립경균일，외관원정；평균립경위（178.5±0.8）nm，PDI위（0.214±0.013），Zeta전위위-（38.47±0.46）mV，초려리심법측정재약납미립적포봉솔위（48.85±0.66）％，재약량위（4.79±0.13）％；선택10％적감로순위동간보호제，복용후득도구유람색유광적립경균일적납미립혼현액。결론구기화투명질산납미립시단백다태류약물구복급약적잠재재체，위하일보연구이도소납미립재대서체내약효、약동학연구제공전제화기출。
Objective To prepare insulin thiolated hyaluronic acid nanoparticles (Ins-HA-Cys-NPs)and study its physicochemical properties. Methods The Ins-HA-Cys-NPs was prepared by ultrasonic emulsifying method,and the properties of nanoparticles including morphology,mean diameter,Zeta potential,entrapment efficiency and drug loading efficiency were studied,as well as the cryoprotectant selection.Results The prepared nanoparticles was round in appearance and the mean diameter was(178.5 ±0.8)nm,the polydispersity index was (0.214 ±0.013)and the Zeta potential was -(38.47 ±0.46 )mV,while the entrapment efficiency was (48.85 ±0.66 )%,drug loading efficiency was (4.79 ±0.13 )%;10%mannitol as cryoprotectant provided uniform and well dispersed suspension of nanoparticles with blue opalescence after redispersion.Conclusion The thiolated hyaluronic acid nanoparticles may be used as the carrier for oral drug delivery system of insulin,and it provides a basis for studies on rats in vivo.