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Background <p>The oral delivery of peptide and protein therapeutics remains a significant challenge due to inherent physicochemical limitations, enzymatic degradation, and limited gastrointestinal (GI) absorption. These biomolecules, though highly potent, often suffer from low bioavailability, necessitating parental administration that impairs patient compliance.</p> Main Body of the Abstract <p>This review systematically addresses the multifaceted barriers impeding oral peptide delivery, including size, charge, polarity, enzymatic breakdown, efflux transporters, and tight junction restrictions. Strategies to overcome these challenges are critically discussed, encompassing absorption enhancers, protease inhibitors, cyclization, PEGylation, lipidation, and mucoadhesive systems. Advances in formulation technologies such as nanoparticles, liposomes, SLNs, micro/nanoemulsions, and gastro-retentive systems are evaluated for their role in protecting peptides and enhancing intestinal uptake. Emerging targeting approaches, including M cells, FcRn, and PepT1-mediated delivery, are also explored. Furthermore, the integration of computational modeling and molecular docking is highlighted as a transformative tool for excipient compatibility, conjugate design, and prediction of formulation behavior.</p> Short Conclusion <p>Together, these innovations demonstrate the potential for successful oral peptide therapeutics and represent a pivotal shift toward patient-friendly drug delivery systems. This review provides a comprehensive, updated synthesis that will aid researchers and formulation scientists in designing next-generation oral peptide delivery systems.</p>

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Oral Peptide Delivery Reimagined: Molecular Barriers, Formulation Strategies, and the Rise of Computational Design

  • 期刊论文

  • 发表日期：

    2025年9月29日

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  • Shailesh D. Dadge,
  • Shivam Mishra,
  • Sharib Khan,
  • Shubhi Yadav,
  • Rabi Sankar Bhatta,
  • Jiaur R. Gayen

摘要

Background

The oral delivery of peptide and protein therapeutics remains a significant challenge due to inherent physicochemical limitations, enzymatic degradation, and limited gastrointestinal (GI) absorption. These biomolecules, though highly potent, often suffer from low bioavailability, necessitating parental administration that impairs patient compliance.

Main Body of the Abstract

This review systematically addresses the multifaceted barriers impeding oral peptide delivery, including size, charge, polarity, enzymatic breakdown, efflux transporters, and tight junction restrictions. Strategies to overcome these challenges are critically discussed, encompassing absorption enhancers, protease inhibitors, cyclization, PEGylation, lipidation, and mucoadhesive systems. Advances in formulation technologies such as nanoparticles, liposomes, SLNs, micro/nanoemulsions, and gastro-retentive systems are evaluated for their role in protecting peptides and enhancing intestinal uptake. Emerging targeting approaches, including M cells, FcRn, and PepT1-mediated delivery, are also explored. Furthermore, the integration of computational modeling and molecular docking is highlighted as a transformative tool for excipient compatibility, conjugate design, and prediction of formulation behavior.

Short Conclusion

Together, these innovations demonstrate the potential for successful oral peptide therapeutics and represent a pivotal shift toward patient-friendly drug delivery systems. This review provides a comprehensive, updated synthesis that will aid researchers and formulation scientists in designing next-generation oral peptide delivery systems.