胰岛素含片或将问世:与注射效果相同

日期:2022-09-05 来源:Scientific Reports

对于许多糖尿病人而言,每天注射胰岛素令人厌烦,而目前大多数口服胰岛素吸收慢,并且大部分被分解浪费。

近日,来自加拿大英属哥伦比亚大学的研究人员正在致力于开发一种口含胰岛素片以替代日常的注射胰岛素,并且取得了突破性进展。最新研究显示,这种口含胰岛素片在小鼠身上的试验效果和注射胰岛素效果相同。相关研究已经发表在近日的《Scientific Reports》杂志上。

这种胰岛素含片利用了一种名为高负荷胰岛素纳米颗粒技术,科学家用粒径318纳米的纳米颗粒负载胰岛素,并制成含片。这种含片并非直接吞服,而是像西瓜霜含片一样放在牙龈和脸颊之间进行溶解,利用口内的粘膜直接将胰岛素输送到肝脏,并且在此过程中不会分解浪费。在小鼠实验中,含片与注射剂吸收方式相同,吸收时间约半小时,持续时长达2~4小时。几乎所有胰岛素都进入了肝脏,在胃中检测不到胰岛素成分。不过,这项成果还没有进行人体试验。这也是下一步的研究计划,一旦成功,全球约5亿糖尿病病人将因此得到生活质量的极大改善。


Scientific Reports


Production of high loading insulin nanoparticles suitable for oral delivery by spray drying and freeze drying techniques

Abstract

Insulin nanoparticles (NPs) with high loading content have found diverse applications in different dosage forms. This work aimed to evaluate the impact of freeze-drying and spray drying process on the structures of insulin-loaded chitosan nanoparticles, with or without mannitol as cryoprotectants. We also assessed the quality of these nanoparticles by redissolving them. Before dehydration, the chitosan/sodium tripolyphosphate/insulin crosslinked nanoparticles were optimized to 318 nm of particle size, 0.18 of PDI, 99.4% of entrapment efficiency, and 25.01% of loading content. After reconstitution, all nanoparticles, except the one produced by the freeze-drying method without using mannitol, maintained their spherical particle structure. The nanoparticles dehydrated by spray drying without mannitol also showed the smallest mean particle size (376 nm) and highest loading content (25.02%) with similar entrapment efficiency (98.7%) and PDI (0.20) compared to mannitol-containing nanoparticles dehydrated by either spray drying or freeze-drying techniques. The nanoparticles dried by spray drying without mannitol also resulted in the fastest release and highest cellular uptake efficacy of insulin. This work shows that spray drying can dehydrate insulin nanoparticles without the need for cryoprotectants, creating a significant advantage in terms of greater loading capacity with lower additive requirements and operating costs as compared to conventional freeze drying approaches.


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编校:马 曦

审核:邹小勇


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