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Application of penetration enhancers in oral peptide drugs
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Xin-yu ZHOU1, Dong-shuai SHANG1, Ya-nan JIN1, Quan-jin WANG1, Guang-pu LIU2, *, Kai-ming WANG1, *
Acta Pharmaceutica Sinica | 2026, 61(6) : 2108 - 2122
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Acta Pharmaceutica Sinica | 2026, 61(6): 2108-2122
• Reviews •
Application of penetration enhancers in oral peptide drugs
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Xin-yu ZHOU1, Dong-shuai SHANG1, Ya-nan JIN1, Quan-jin WANG1, Guang-pu LIU2, *, Kai-ming WANG1, *
Affiliations
  • 1School of Biological Science and Technology, University of Jinan, Jinan 250022, China
  • 2Department of Pharmacy, Qilu Hospital of Shandong University, Jinan 250012, China
Published: 2026-06-12 doi: 10.16438/j.0513-4870.2025-1042
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Peptide therapeutics are characterized by high potency, exquisite specificity, and low toxicity, and have therefore been widely adopted for the clinical management of diverse diseases. However, their inherently low gastrointestinal permeability, rapid enzymatic degradation, and multiple physiological barriers collectively result in extremely low oral bioavailability, necessitating parenteral administration. Compared with the more convenient and patient-compliant oral route, chronic injection is associated with poor adherence and an increased incidence of adverse reactions. In recent years, extensive research has focused on permeation enhancers (PEs) based strategies to improve the oral bioavailability of peptide drugs. This review systematically summarizes the mechanisms of action and clinical applications of representative PEs-including surfactants (sodium caprylate, sodium caprate, alkyl glycosides, bile salts), chelating agents, chitosan and cell-penetrating peptides. It also summarizes related patented technologies (EligenTM, TPETM, GIPETTM, PODTM, PeptelligenceTM) to facilitate the development and clinical translation of oral peptide formulations.

oral peptide drug  /  permeation enhancer  /  mechanisms of action  /  clinical application  /  proprietary technology
周欣雨, 尚东帅, 金亚男, 王泉锦, 刘光璞, 王凯铭. 渗透增强剂在口服肽类药物中的应用. 药学学报, 2026 , 61 (6) : 2108 -2122 . DOI: 10.16438/j.0513-4870.2025-1042
Xin-yu ZHOU, Dong-shuai SHANG, Ya-nan JIN, Quan-jin WANG, Guang-pu LIU, Kai-ming WANG. Application of penetration enhancers in oral peptide drugs[J]. Acta Pharmaceutica Sinica, 2026 , 61 (6) : 2108 -2122 . DOI: 10.16438/j.0513-4870.2025-1042
Year 2026 volume 61 Issue 6
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120
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Article Info
doi: 10.16438/j.0513-4870.2025-1042
  • Receive Date:2025-09-02
  • Online Date:2026-09-21
  • Published:2026-06-12
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History
  • Received:2025-09-02
  • Revised:2026-01-08
Affiliations
    1School of Biological Science and Technology, University of Jinan, Jinan 250022, China
    2Department of Pharmacy, Qilu Hospital of Shandong University, Jinan 250012, China
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表12种不同金属材料的力学参数
科
Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)
属
Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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