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  • Zwitterionic micelles efficiently deliver oral insulin without opening tight junctions.

Zwitterionic micelles efficiently deliver oral insulin without opening tight junctions.

Nature nanotechnology (2020-06-03)
Xiangfei Han, Yang Lu, Jinbing Xie, Ershuai Zhang, Hui Zhu, Hong Du, Ke Wang, Boyi Song, Chengbiao Yang, Yuanjie Shi, Zhiqiang Cao
ABSTRACT

Oral delivery of protein drugs is considered a life-changing solution for patients who require regular needle injections. However, clinical translation of oral protein formulations has been hampered by inefficient penetration of drugs through the intestinal mucus and epithelial cell layer, leading to low absorption and bioavailability, and safety concerns owing to tight junction openings. Here we report a zwitterionic micelle platform featuring a virus-mimetic zwitterionic surface, a betaine side chain and an ultralow critical micelle concentration, enabling drug penetration through the mucus and efficient transporter-mediated epithelial absorption without the need for tight junction opening. This micelle platform was used to fabricate a prototype oral insulin formulation by encapsulating a freeze-dried powder of zwitterionic micelle insulin into an enteric-coated capsule. The biocompatible oral insulin formulation shows a high oral bioavailability of >40%, offers the possibility to fine tune insulin acting profiles and provides long-term safety, enabling the oral delivery of protein drugs.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Lactate Dehydrogenase Activity Assay Kit, sufficient for 500 colorimetric tests
Sigma-Aldrich
3-Sulfopropyl methacrylate potassium salt, 98%