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新型微针注射器可用于口服递送大分子
2019-10-09 11:07

美国麻省理工学院Giovanni Traverso和Robert Langer等研究人员合作开发了可用于大分子口服递送的腔内展开微针注射器。2019年10月7日,《自然—医学》在线发表了这项成果。

研究人员开发了一种称为腔内展开微针注射器的可吸收胶囊,其通过使用一组展开臂将可溶解药物的微针快速推进肠道组织,从而可以口服递送生物药物。在人体外和猪体内的研究表明,该设备始终将微针递送至组织,而不会引起完全的厚度穿孔。使用胰岛素作为模型药物,研究人员发现,当胶囊启动时,管腔展开微针注射器在4小时的采样时间内提供了较快的药代动力学吸收曲线,并且其皮下注射的系统吸收率比皮下注射高出10%。因为具有装载多种微针配方的能力,该设备可以用作口服治疗剂量的大分子药物平台。

研究人员表示,胰岛素和其他可注射生物药物已经改变了对患糖尿病患者的治疗,但是患者和医疗保健提供者通常更喜欢使用并开出口服效果不佳的药物。与皮下给药的药物相比,口服制剂可减少患者不适,在高温下显示出更高的化学稳定性,并且不会产生生物危害性的针头废物。生物药物的口服剂型是理想的。但是,大分子药物不易通过胃肠道吸收到血液中。

附:英文原文

Title: A luminal unfolding microneedle injector for oral delivery of macromolecules

Author: Alex Abramson, Ester Caffarel-Salvador, Vance Soares, Daniel Minahan, Ryan Yu Tian, Xiaoya Lu, David Dellal, Yuan Gao, Soyoung Kim, Jacob Wainer, Joy Collins, Siddartha Tamang, Alison Hayward, Tadayuki Yoshitake, Hsiang-Chieh Lee, James Fujimoto, Johannes Fels, Morten Revsgaard Frederiksen, Ulrik Rahbek, Niclas Roxhed, Robert Langer, Giovanni Traverso

Issue&Volume: 2019-10-07

Abstract: Insulin and other injectable biologic drugs have transformed the treatment of patients suffering from diabetes1,2, yet patients and healthcare providers often prefer to use and prescribe less effective orally dosed medications35. Compared with subcutaneously administered drugs, oral formulations create less patient discomfort4, show greater chemical stability at high temperatures6, and do not generate biohazardous needle waste7. An oral dosage form for biologic medications is ideal; however, macromolecule drugs are not readily absorbed into the bloodstream through the gastrointestinal tract8. We developed an ingestible capsule, termed the luminal unfolding microneedle injector, which allows for the oral delivery of biologic drugs by rapidly propelling dissolvable drug-loaded microneedles into intestinal tissue using a set of unfolding arms. During ex vivo human and in vivo swine studies, the device consistently delivered the microneedles to the tissue without causing complete thickness perforations. Using insulin as a model drug, we showed that, when actuated, the luminal unfolding microneedle injector provided a faster pharmacokinetic uptake profile and a systemic uptake >10% of that of a subcutaneous injection over a 4-h sampling period. With the ability to load a multitude of microneedle formulations, the device can serve as a platform to orally deliver therapeutic doses of macromolecule drugs. A luminal unfolding microneedle injector device (LUMI) is engineered as a custom capsule capable of efficient biologic macromolecular drug delivery into the bloodstream via selective deployment within the gastrointestinal tract.

DOI: 10.1038/s41591-019-0598-9

Source:https://www.nature.com/articles/s41591-019-0598-9

Nature Medicine:《自然—医学》,创刊于1995年。隶属于施普林格·自然出版集团,最新IF:87.241
官方网址:https://www.nature.com/nm/
投稿链接:https://mts-nmed.nature.com/cgi-bin/main.plex


本期文章:《自然—医学》:Online/在线发表

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