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Research progress in oral targeted delivery systems for macromolecular drugs
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Zheng ZHENG1, 2, 3, Ya-wen ZHANG2, 3, Yong-bo SONG1, *, Wu-fa FAN2, 3, *
Acta Pharmaceutica Sinica | 2026, 61(5) : 1560 - 1572
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Acta Pharmaceutica Sinica | 2026, 61(5): 1560-1572
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Research progress in oral targeted delivery systems for macromolecular drugs
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Zheng ZHENG1, 2, 3, Ya-wen ZHANG2, 3, Yong-bo SONG1, *, Wu-fa FAN2, 3, *
Affiliations
  • 1College of Life Sciences and Biopharmaceuticals, Shenyang Pharmaceutical University, Benxi 117000, China
  • 2State Key Laboratory of Active Substances and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
  • 3Beijing Key Laboratory of Drug Delivery Technology and Novel Formulation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2026-05-12 doi: 10.16438/j.0513-4870.2025-1333
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Macromolecular drugs, due to their high specificity and excellent biological activity, play a crucial role in disease treatment. The oral administration route, with its advantages of high patient compliance and safety, is considered an ideal approach for delivering macromolecular drugs. However, various biological barriers in the gastrointestinal tract significantly limit the oral bioavailability and targeted delivery efficiency of macromolecular drugs. Existing research has primarily focused on overcoming single barriers or designing single carriers, this paper systematically addresses the multiple biological barriers encountered during the targeted delivery of orally administered macromolecular drugs. It provides an overview of various nanocarriers suitable for the targeted oral delivery of macromolecular drugs and delves into the latest advances in organ-specific targeting strategies, offering new perspectives for the precision treatment of orally administered macromolecular drugs. Furthermore, it incorporates examples of applications involving macromolecular drugs such as peptides, proteins, and nucleic acids, providing theoretical insights and research directions for enhancing the oral delivery efficiency of macromolecular drugs.

macromolecular drug  /  oral delivery  /  nanoscale drug delivery system  /  biological barrier  /  bioavailability
郑正, 张雅文, 宋永波, 范武发. 口服大分子药物靶向递送研究进展. 药学学报, 2026 , 61 (5) : 1560 -1572 . DOI: 10.16438/j.0513-4870.2025-1333
Zheng ZHENG, Ya-wen ZHANG, Yong-bo SONG, Wu-fa FAN. Research progress in oral targeted delivery systems for macromolecular drugs[J]. Acta Pharmaceutica Sinica, 2026 , 61 (5) : 1560 -1572 . DOI: 10.16438/j.0513-4870.2025-1333
Year 2026 volume 61 Issue 5
308
153
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doi: 10.16438/j.0513-4870.2025-1333
  • Receive Date:2025-11-11
  • Online Date:2026-09-21
  • Published:2026-05-12
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History
  • Received:2025-11-11
  • Revised:2026-01-05
Affiliations
    1College of Life Sciences and Biopharmaceuticals, Shenyang Pharmaceutical University, Benxi 117000, China
    2State Key Laboratory of Active Substances and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
    3Beijing Key Laboratory of Drug Delivery Technology and Novel Formulation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, 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
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Percentage of
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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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