中国生化药物杂志
中國生化藥物雜誌
중국생화약물잡지
CHINESE JOURNAL OF BIOCHEMICAL PHARMACEUTICS
2014年
1期
79-81
,共3页
刘智强%陈旭东%龙方懿%祝慧凤
劉智彊%陳旭東%龍方懿%祝慧鳳
류지강%진욱동%룡방의%축혜봉
胰岛素%纳米粒%降糖作用%多肽
胰島素%納米粒%降糖作用%多肽
이도소%납미립%강당작용%다태
insulin%nanoparticles%hypoglycemic effect%peptide
目的：构建黏膜细胞特异性多肽（CSK）修饰的载胰岛素（insulin，INS）口服纳米粒（CSK-INS-NPs），并对其体外性质以及体内降血糖效果进行评价。方法用复乳法制备CSK修饰的载胰岛素聚乳酸羟基乙酸（poly lactic-co-glycolic acid，PLGA）纳米粒，对其理化性质和包封率进行考察。通过体外人克隆结肠腺癌细胞（Caco-2）摄取实验考察CSK修饰的纳米粒的细胞穿透能力和跨膜能力。构建糖尿病模型大鼠评价口服纳米粒的降血糖能力。结果制备得到的CSK-INS-NPs粒径为（134.4±15）nm ，粒径多分散系数小于0.3，胰岛素的包封率（EE%）为71%。体外Caco-2细胞摄取实验表明，细胞对CSK-INS-NPs摄取量是INS-NPs的2.8倍。相比于INS-NPs，CSK-INS-NPs能够更加高效的穿透Caco-2细胞层。糖尿病大鼠的降糖实验表明，在10 h内，口服CSK-INS-NPs能够降低血糖浓度，且保持稳定。结论 CSK能够促进载胰岛素纳米粒跨越Caco-2细胞膜，CSK-INS-NPs是一种潜在的高效口服胰岛素载体给药系统。
目的：構建黏膜細胞特異性多肽（CSK）脩飾的載胰島素（insulin，INS）口服納米粒（CSK-INS-NPs），併對其體外性質以及體內降血糖效果進行評價。方法用複乳法製備CSK脩飾的載胰島素聚乳痠羥基乙痠（poly lactic-co-glycolic acid，PLGA）納米粒，對其理化性質和包封率進行攷察。通過體外人剋隆結腸腺癌細胞（Caco-2）攝取實驗攷察CSK脩飾的納米粒的細胞穿透能力和跨膜能力。構建糖尿病模型大鼠評價口服納米粒的降血糖能力。結果製備得到的CSK-INS-NPs粒徑為（134.4±15）nm ，粒徑多分散繫數小于0.3，胰島素的包封率（EE%）為71%。體外Caco-2細胞攝取實驗錶明，細胞對CSK-INS-NPs攝取量是INS-NPs的2.8倍。相比于INS-NPs，CSK-INS-NPs能夠更加高效的穿透Caco-2細胞層。糖尿病大鼠的降糖實驗錶明，在10 h內，口服CSK-INS-NPs能夠降低血糖濃度，且保持穩定。結論 CSK能夠促進載胰島素納米粒跨越Caco-2細胞膜，CSK-INS-NPs是一種潛在的高效口服胰島素載體給藥繫統。
목적：구건점막세포특이성다태（CSK）수식적재이도소（insulin，INS）구복납미립（CSK-INS-NPs），병대기체외성질이급체내강혈당효과진행평개。방법용복유법제비CSK수식적재이도소취유산간기을산（poly lactic-co-glycolic acid，PLGA）납미립，대기이화성질화포봉솔진행고찰。통과체외인극륭결장선암세포（Caco-2）섭취실험고찰CSK수식적납미립적세포천투능력화과막능력。구건당뇨병모형대서평개구복납미립적강혈당능력。결과제비득도적CSK-INS-NPs립경위（134.4±15）nm ，립경다분산계수소우0.3，이도소적포봉솔（EE%）위71%。체외Caco-2세포섭취실험표명，세포대CSK-INS-NPs섭취량시INS-NPs적2.8배。상비우INS-NPs，CSK-INS-NPs능구경가고효적천투Caco-2세포층。당뇨병대서적강당실험표명，재10 h내，구복CSK-INS-NPs능구강저혈당농도，차보지은정。결론 CSK능구촉진재이도소납미립과월Caco-2세포막，CSK-INS-NPs시일충잠재적고효구복이도소재체급약계통。
Objective To investigate the effects of CSK-conjugated PLGA nanoparticles on oral delivery of insulin in vitro and in vivo.Method CSK-INS-NPs were prepared by double-emulsion. Nanoparticle size、zeta potential and entrapment efficiency were measured. The efficiency of cellular uptake on Caco-2 cells in vitro was evaluated. The hypoglycemic effects were evaluated by monitoring the glucose levels in diabetic rats. Results The average sizes was(134. 4 ± 15)nm and their PDI values were less than 0.3.The insulin entrapment efifciency was around 71%. The cellular uptake of CSK-INS-NPs by Caco-2 cells was 2.8 times higher than INS-NPs. The CSK-INS-NPs transferred more insulin across the Caco-2 cell monolayer than INS-NPs and insulin solution did. In vivo experiments,the CSK-INS-NPs could reduce the blood glucose level of diabetic rats after oral administration in 10 h.Conclusion Compared with insulin solution,CSK-INS-NPs enhanced the insulin through Caco-2 cell monolayer by transcellular pathway and may be a potential delivery system for Oral Delivery of Insulin.
