Cited by 5Phytochemicals and Antioxidant ActivitiesNatural Antidiabetic Agents StudiesPhytochemistry and Biological Activities

Research progress on the molecular mechanisms of chlorogenic acid’s pharmacological effects and its advanced drug delivery systems

Open access
Gao, Linran, Zhang, Tianci, Zhang, Xianyu, Ding, Wenbo, Yang, Jianyu, Luo, Yu, Wang, Jingjing, Yuan, Xin +1 more·2026·Frontiers in Pharmacology

Abstract

Chlorogic acid (CGA), a prevalent polyphenol formed in plants, is recognized for its broad spectrum of biological activities, including potent antioxidant, anti-inflammatory, antimicrobial, andmetabolic regulatory effects. This review synthesizes evidence demonstrating CGA’s therapeutic potential across various conditions, such as hypertension, gout, atherosclerosis, and metabolic disorders. Key mechanisms involve neutralizing reactive oxygen species, modulating critical signaling pathways like TLR2/NF-κB and MAPK, enhancing insulin sensitivity, and influencing endothelial function by boosting NO production via eNOS phosphorylation. Despite these promising attributes, CGA’s clinical translation is hindered by significant bioavailability challenges stemming from poor solubility, rapid metabolism, and instability in physiological environments. To address these limitations, innovative drug delivery systems are being investigated. These systems, including polymeric nanoparticles, liposomes, micelles, and hydrogels, offer strategies to encapsulate CGA, thereby protecting it from degradation, improving its dissolution properties, and enabling controlled or targeted release at specific sites of action. Such advancements in delivery technology are crucial for enhancing CGA’s stability and bioavailability, ultimately bridging the gap between its demonstrated in vitro and preclinical efficacy and its realization as an effective therapeutic agent in human medicine.

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Crossref · 10.3389/fphar.2026.1746172

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Authors
Gao, L., Zhang, T., Zhang, X., Ding, W., Yang, J., Luo, Y., Wang, J., Yuan, X., & Zhao, Y.
Affiliations
Beihua University (CN)
Corresponding author
Zhao, Yundong
Venue
Frontiers in Pharmacology
Published
2026-03-18
Volume
17
Pages
1746172-1746172
ISSN
1663-9812 (ISSN-L)
OpenAlex
W7138894065
Cited by
4
References
137
Citations by year
2026: 4
FWCI
2.79
Type
journal article
Language
en
Open access
Locations
  • Frontiers in Pharmacology (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Funders
  • People's Government of Jilin Province
  • Beihua University
Topics
  • Health Sciences › Medicine › Biochemistry › Phytochemicals and Antioxidant Activities
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Natural Antidiabetic Agents Studies
  • Life Sciences › Agricultural and Biological Sciences › Plant Science › Phytochemistry and Biological Activities
Keywords
chlorogenic acid, polyphenols, antioxidant activity, anti-inflammatory activity, antimicrobial activity, hypertension, gout, atherosclerosis, metabolic disorders, reactive oxygen species, MAPK signaling, insulin sensitivity, endothelial function, nitric oxide, bioavailability, drug delivery systems, polymeric nanoparticles, liposomes, micelles, hydrogels, controlled release

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