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The dilemma and breakthrough of oral administration of insulin
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Sheng-yu YAO1, Xing-yan FAN1, Kuan JIANG1, Yang HU1, Gang WEI1, 3, 4, *, Yong GAN2, Wei-yue LU1, 3
Acta Pharmaceutica Sinica | 2020, 55(7) : 1549 - 1561
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Acta Pharmaceutica Sinica | 2020, 55(7): 1549-1561
• Reviews •
The dilemma and breakthrough of oral administration of insulin
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Sheng-yu YAO1, Xing-yan FAN1, Kuan JIANG1, Yang HU1, Gang WEI1, 3, 4, *, Yong GAN2, Wei-yue LU1, 3
Affiliations
  • 1. Key Laboratory of Smart Drug Delivery, Ministry of Education, School of Pharmacy, Fudan University, Shanghai 201203, China
  • 2. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
  • 3. The Institutes of Integrative Medicine of Fudan University, Shanghai 200040, China
  • 4. Shanghai Engineering Re-search Center of ImmunoTherapeutics, Shanghai 201203, China
Published: 2020-07-12 doi: 10.16438/j.0513-4870.2020-0913
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Diabetes is characterized by hyperglycemia, resulting from insulin deficiency or resistance, or both. Insulin plays an irreplaceable role in the treatment of diabetes. Subcutaneous injection is the main route of insulin administration, but usually leads to poor compliance and many side effects. Oral insulin is safer and more convenient, which has always been the Holy Grail for people to explore. After oral administration, insulin is absorbed into the hepatic portal vein and transported to the liver, which can activate the normal physiological functions and reduce the risk of hypoglycemia, insulin resistance, and improve patient compliance. However, the gastrointestinal tract has multiple absorption barriers such as chemical barrier, enzyme barrier, and permeation barrier. Due to the physical and chemical properties of insulin, it is difficult to achieve desired oral bioavailability. This article reviews the recent attempts and progress in the field of oral administration of insulin driven by innovative drug delivery technologies and biomaterials, including structural modification, enzyme inhibitors, absorption enhancers, various nanoparticles, liposomes, microspheres, and even microorganisms. Some clinical researches on oral insulin are also introduced.

diabetes mellitus  /  insulin  /  oral administration  /  bioavailability  /  drug delivery system  /  intestinal absorption
Sheng-yu YAO, Xing-yan FAN, Kuan JIANG, Yang HU, Gang WEI, Yong GAN, Wei-yue LU. The dilemma and breakthrough of oral administration of insulin[J]. Acta Pharmaceutica Sinica, 2020 , 55 (7) : 1549 -1561 . DOI: 10.16438/j.0513-4870.2020-0913
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Article Info
doi: 10.16438/j.0513-4870.2020-0913
  • Receive Date：2020-06-07
  • Online Date：2026-01-21
  • Published：2020-07-12
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History
  • Received：2020-06-07
  • Revised：2020-06-13
Funding
Affiliations
    1. Key Laboratory of Smart Drug Delivery, Ministry of Education, School of Pharmacy, Fudan University, Shanghai 201203, China
    2. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
    3. The Institutes of Integrative Medicine of Fudan University, Shanghai 200040, China
    4. Shanghai Engineering Re-search Center of ImmunoTherapeutics, Shanghai 201203, China
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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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