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A self-unfolding polymer foil loaded with a permeation enhancer Ionogel for superior oral peptide delivery

delete2026-07-23
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OA
AI
K
Konstantinos Raptis
R
R E McCabe
M
Marta Rubio-Huertas
S
Stine Rønholt
L
Lasse Saaby
L
Lasse Højlund Eklund Thamdrup
M
Mahdi Ghavami
K
Khorshid Kamguyan
H
Hanne Mørck Nielsen *
A
Anja Boisen *
DOI:10.1007/s13346-026-02179-6delete
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Abstract

Abstract

En 中文
Peptide drugs have gained considerable attention as new molecular entities, due to their high target specificity. However, oral delivery of peptides remains a major challenge, and current formulation approaches typically achieve only low single-digit bioavailability, prompting exploration of synergistic strategies to improve absorption. In this work, a self-unfolding foil device, designed for unidirectional drug release in close proximity to the intestinal mucosa, is combined with a potent permeation enhancer-based ionogel formulation for exploitation of synergies from two different oral delivery approaches. The choline decanoate ionogel is loaded into the foil, and insulin release optimized through hydrophilic surface modification and tailored cavity design. In vivo evaluation in rats demonstrate a bioavailability of 12.5% and a biopotency of 20% relative to subcutaneous administration representing approximately three- and four-fold increases, respectively, compared with the formulation control group. These findings demonstrate that unidirectional release from an advanced drug delivery system can markedly enhance formulation performance and pave the way for further development of similar combinatorial delivery strategies. Overall, this study reports the highest insulin bioavailability achieved with the self-unfolding foil platform to date, and among the highest reported in literature, highlighting its promise for advancing oral peptide delivery in future preclinical studies.
Keywords:
Oral peptide therapeutic
Drug delivery
Device
Ionic liquid
Self-unfolding foil

Journal

Drug Delivery and Translational Research cover
Drug Delivery and Translational Research
IF:
5.5
Papers:
2.2K
Citations:
7.4K

Organization

F
Faculty of Health and Medical Sciences
Scholars:
353
Papers: 142
Citations: 2
D
Department of Health Technology
Scholars:
27
Papers: 12
Citations: 0
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