磺基甜菜碱修饰纤维素纳米晶口服胰岛素递送系统的构建与性能评价  

An efficient insulin delivery system based on cellulose nanocrystals

作　　者：王欣然 孙红男[1] 木泰华[1] WANG Xinran;SUN Hongnan;MU Taihua(Institute of Food Science and Technology,Chinese Academy of Agricultural Sciences,Key Laboratory of Agro-Products Processing,Ministry of Agriculture and Rural Affairs,Beijing 100193,China)

机构地区：[1]中国农业科学院农产品加工研究所农业农村部农产品加工综合性重点实验室,北京100193

出　　处：《应用化工》2025年第2期375-382,共8页Applied Chemical Industry

基　　金：中国农业科学院科技创新工程(CAAS-ASTIP-202X-IFST)。

摘　　要：实现胰岛素的口服递送是糖尿病患者减轻注射疼痛、改善生活质量的希望。然而,由于胃肠道吸收屏障的存在,目前口服胰岛素的生物利用度低,阻碍了商业化目标的实现。制备了叶酸修饰的锌金属有机框架(MOF)和磺基甜菜碱修饰纤维素纳米晶(CS)作为胰岛素(Ins)的包埋材料,开发了口服胰岛素(Ins@MOF@CS)。Ins@MOF@CS的胰岛素包封率(97.38±0.09)%,载药量(27.54±0.03)%。体外释放试验中,经过6 h的模拟肠液孵育,Ins@MOF@CS释放了(73.87±0.57)%的胰岛素。Ins@MOF@CS被Caco-2细胞摄取的效率显著高于游离胰岛素(p<0.05),其表观渗透系数是游离胰岛素的3.46倍。此外,Ins@MOF@CS具有高生物相容性。Ins@MOF@CS可能是一种潜在的提高胰岛素生物利用度的口服递送系统。To realize clinical insulin oral delivery is the hope for diabetes patients to reduce injection pain and improve quality of life.However,due to the presence of gastrointestinal absorption barriers,the current low bioavailability of oral insulin hinders the achievement of commercial goals.The folate modified zinc metal organic frameworks(MOF)and sulfobetaine modified cellulose nanocrystals(CS)were prepared as embedding materials for insulin(Ins),and oral insulin(Ins@MOF@CS)was developed.The insulin encapsulation rate of Ins@MOF@CS was(97.38±0.09)%,and the drug loading was(27.54±0.03)%.In vitro release test,after 6 h of simulated intestinal fluid incubation,Ins@MOF@CS released(73.87±0.57)%insulin.The efficiency of Ins@MOF@CS uptake by Caco-2 cells was significantly higher than that of insulin(p<0.05),and the apparent permeability coefficient was 3.46 times that of free insulin.In addition,Ins@MOF@CS had high biocompatibility.Ins@MOF@CS may be a potential oral delivery system for improving insulin bioavailability.

关 键 词：金属有机框架 纤维素纳米晶 口服胰岛素 水凝胶 两性离子 

分 类 号：TQ427.26[化学工程] TQ460.4