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Research progress of histidine-based tumor-targeting drug delivery systems
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Meng JI, Da-li CHEN, Jia-sheng TU*, Chun-meng SUN*
Acta Pharmaceutica Sinica | 2022, 57(1) : 64 - 75
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Acta Pharmaceutica Sinica | 2022, 57(1): 64-75
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Research progress of histidine-based tumor-targeting drug delivery systems
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Meng JI, Da-li CHEN, Jia-sheng TU*, Chun-meng SUN*
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  • NMPA Key Laboratory for Research and Evaluation of Pharmaceutical Preparations and Excipients, Center for Research Development and Evaluation of Pharmaceutical Excipients and Generic Drugs, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
Published: 2022-01-12 doi: 10.16438/j.0513-4870.2021-1174
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As a basic amino acid, histidine has a pKa close to the acidity of the tumor microenvironment, thus the charge and solubility of histidine are able to vary as the pH changes. Under a neutral environment, histidine is not charged and exhibits hydrophobic properties, while it can be protonated and becomes hydrophilic when exposed to mildly acidic pH, such as tumor microenvironment. Therefore, histidine is widely used in the design of drug delivery systems to target the mildly acidic pH of tumor microenvironment. This article reviews the recent progresses of histidine-based tumor-targeting drug delivery systems, and summarizes the principles on promoting internalization and tuning drug release by taking advantage of histidine. Finally, we point out the common issues on histidine application and illustrate its future prospects.

histidine  /  cell-penetrating peptide  /  tumor microenvironment  /  drug delivery system  /  therapy
Meng JI, Da-li CHEN, Jia-sheng TU, Chun-meng SUN. Research progress of histidine-based tumor-targeting drug delivery systems[J]. Acta Pharmaceutica Sinica, 2022 , 57 (1) : 64 -75 . DOI: 10.16438/j.0513-4870.2021-1174
Year 2022 volume 57 Issue 1
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doi: 10.16438/j.0513-4870.2021-1174
  • Receive Date:2021-08-11
  • Online Date:2025-12-22
  • Published:2022-01-12
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  • Received:2021-08-11
  • Revised:2021-09-08
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    NMPA Key Laboratory for Research and Evaluation of Pharmaceutical Preparations and Excipients, Center for Research Development and Evaluation of Pharmaceutical Excipients and Generic Drugs, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

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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