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Intelligent Escape System for the Oral Delivery of Liraglutide: A Perfect Match for Gastrointestinal Barriers.
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2020-04-08 , DOI: 10.1021/acs.molpharmaceut.9b01307 Miaomiao Yin 1 , Yina Song 2 , Shiqi Guo 1 , Xuemei Zhang 2 , Kaoxiang Sun 1, 2 , Youxin Li 1, 2 , Yanan Shi 3
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2020-04-08 , DOI: 10.1021/acs.molpharmaceut.9b01307 Miaomiao Yin 1 , Yina Song 2 , Shiqi Guo 1 , Xuemei Zhang 2 , Kaoxiang Sun 1, 2 , Youxin Li 1, 2 , Yanan Shi 3
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Epithelial cells are known to impede the oral delivery of polypeptides, and the accumulation of mucus and regular dynamic renewal also significantly impede drug absorption. In this work, we prepared a core–shell (COS) nanosystem using poly-N-(2-hydroxypropyl)methacrylamide (pHPMA)/chitosan (CTS). Liraglutide (NN2211) was isolated from the gastrointestinal environment and smoothly passes through the mucous layer. CSKSSDYQC (CSK) peptide and hemagglutinin-2 (HA2) were introduced into the COS nanosystem to establish a complete path from the oral cavity to the epithelial basal side. The fate of nanocapsules in vivo was studied by fluorescence detection. The results showed that the nanocapsules escaped smoothly from the mucus. Taking into account the characteristics of CSK targeting goblet cells, we conducted cell-level studies, and the results showed that after the modification of CSK and pHPMA, more nanocapsules entered the cells. In vitro and in vivo evaluation results showed that the system successfully established a complete path from mucus to epithelial cells by responding to the gastrointestinal environment multiple times.
中文翻译：
口服利拉鲁肽的智能逃生系统：胃肠道屏障的完美匹配。
已知上皮细胞阻碍多肽的口服递送，并且粘液的积累和定期动态更新也显着阻碍药物吸收。在这项工作中，我们使用聚N-（2-羟丙基）甲基丙烯酰胺（pHPMA）/壳聚糖（CTS）制备了核-壳（COS）纳米系统。利拉鲁肽（NN2211）从胃肠道环境中分离出来，并顺利通过粘液层。将CSKSSDYQC（CSK）肽和血凝素2（HA 2）引入COS纳米系统，以建立从口腔到上皮基底侧的完整路径。纳米胶囊在体内的命运通过荧光检测进行了研究。结果表明，纳米胶囊从粘液中顺利逸出。考虑到靶向CSK的杯状细胞的特性，我们进行了细胞水平的研究，结果表明，对CSK和pHPMA进行修饰后，更多的纳米胶囊进入了细胞。体外和体内评估结果表明，该系统通过多次响应胃肠道环境，成功建立了从粘液到上皮细胞的完整路径。
更新日期：2020-04-08
中文翻译：
口服利拉鲁肽的智能逃生系统：胃肠道屏障的完美匹配。
已知上皮细胞阻碍多肽的口服递送，并且粘液的积累和定期动态更新也显着阻碍药物吸收。在这项工作中，我们使用聚N-（2-羟丙基）甲基丙烯酰胺（pHPMA）/壳聚糖（CTS）制备了核-壳（COS）纳米系统。利拉鲁肽（NN2211）从胃肠道环境中分离出来，并顺利通过粘液层。将CSKSSDYQC（CSK）肽和血凝素2（HA 2）引入COS纳米系统，以建立从口腔到上皮基底侧的完整路径。纳米胶囊在体内的命运通过荧光检测进行了研究。结果表明，纳米胶囊从粘液中顺利逸出。考虑到靶向CSK的杯状细胞的特性，我们进行了细胞水平的研究，结果表明，对CSK和pHPMA进行修饰后，更多的纳米胶囊进入了细胞。体外和体内评估结果表明，该系统通过多次响应胃肠道环境，成功建立了从粘液到上皮细胞的完整路径。
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