Proteins and peptides (PPs) have gradually become more attractive therapeutic molecules than small molecular drugs due to their high selectivity and efficacy, but fewer side effects. Owing to the poor stability and limited permeability through gastrointestinal (GI) tract and epithelia, the therapeutic PPs are usually administered by parenteral route. Given the big demand for oral administration in clinical use, a variety of researches focused on developing new technologies to overcome GI barriers of PPs, such as enteric coating, enzyme inhibitors, permeation enhancers, nanoparticles, as well as intestinal microdevices. Some new technologies have been developed under clinical trials and even on the market. This review summarizes the history, the physiological barriers and the overcoming approaches, current clinical and preclinical technologies, and future prospects of oral delivery of PPs. (C) 2021 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
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Univ Copenhagen, Fac Hlth & Med Sci, Dept Pharm, Biol Sect, DK-2100 Copenhagen O, DenmarkUniv Copenhagen, Fac Hlth & Med Sci, Dept Pharm, Biol Sect, DK-2100 Copenhagen O, Denmark
Kristensen, M.
Foged, C.
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Univ Copenhagen, Fac Hlth & Med Sci, Dept Pharm, Biol Sect, DK-2100 Copenhagen O, DenmarkUniv Copenhagen, Fac Hlth & Med Sci, Dept Pharm, Biol Sect, DK-2100 Copenhagen O, Denmark
Foged, C.
Berthelsen, J.
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Univ Copenhagen, Fac Hlth & Med Sci, Dept Int Hlth Immunol & Microbiol, DK-2200 Copenhagen N, DenmarkUniv Copenhagen, Fac Hlth & Med Sci, Dept Pharm, Biol Sect, DK-2100 Copenhagen O, Denmark
Berthelsen, J.
Nielsen, H. Morck
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Univ Copenhagen, Fac Hlth & Med Sci, Dept Pharm, Biol Sect, DK-2100 Copenhagen O, DenmarkUniv Copenhagen, Fac Hlth & Med Sci, Dept Pharm, Biol Sect, DK-2100 Copenhagen O, Denmark
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Univ Copenhagen, Dept Pharm, Fac Hlth & Med Sci, DK-2100 Copenhagen O, DenmarkUniv Copenhagen, Dept Pharm, Fac Hlth & Med Sci, DK-2100 Copenhagen O, Denmark
Li, Ping
Nielsen, Hanne Morck
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Univ Copenhagen, Dept Pharm, Fac Hlth & Med Sci, DK-2100 Copenhagen O, DenmarkUniv Copenhagen, Dept Pharm, Fac Hlth & Med Sci, DK-2100 Copenhagen O, Denmark
Nielsen, Hanne Morck
Mullertz, Anette
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Univ Copenhagen, Dept Pharm, Fac Hlth & Med Sci, DK-2100 Copenhagen O, Denmark
Univ Copenhagen, Bioneer FARMA, Fac Hlth & Med Sci, DK-2100 Copenhagen O, DenmarkUniv Copenhagen, Dept Pharm, Fac Hlth & Med Sci, DK-2100 Copenhagen O, Denmark
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Univ British Columbia, Fac Pharmaceut Sci, Vancouver, BC V6T 1Z3, CanadaUniv British Columbia, Fac Pharmaceut Sci, Vancouver, BC V6T 1Z3, Canada
Saxena, Tanya
Sie, Claire
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Univ British Columbia, Fac Pharmaceut Sci, Vancouver, BC V6T 1Z3, CanadaUniv British Columbia, Fac Pharmaceut Sci, Vancouver, BC V6T 1Z3, Canada
Sie, Claire
Lin, Kristine
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Univ British Columbia, Fac Pharmaceut Sci, Vancouver, BC V6T 1Z3, CanadaUniv British Columbia, Fac Pharmaceut Sci, Vancouver, BC V6T 1Z3, Canada
Lin, Kristine
Ye, Daisy
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Univ British Columbia, Fac Pharmaceut Sci, Vancouver, BC V6T 1Z3, CanadaUniv British Columbia, Fac Pharmaceut Sci, Vancouver, BC V6T 1Z3, Canada
Ye, Daisy
Saatchi, Katayoun
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Univ British Columbia, Fac Pharmaceut Sci, Vancouver, BC V6T 1Z3, CanadaUniv British Columbia, Fac Pharmaceut Sci, Vancouver, BC V6T 1Z3, Canada
Saatchi, Katayoun
Hafeli, Urs O.
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Univ British Columbia, Fac Pharmaceut Sci, Vancouver, BC V6T 1Z3, Canada
Univ Copenhagen, Fac Hlth & Med Sci, Dept Pharm, DK-2100 Copenhagen, DenmarkUniv British Columbia, Fac Pharmaceut Sci, Vancouver, BC V6T 1Z3, Canada