Ethnopharmacological relevance Hesperidin is a citrus-derived bioflavonoid that has a variety of pharmacological properties, such as anti-inflammatory, anti-carcinogenic, anti-viral and antioxidant properties. It exhibits effectiveness against gastric, colon, prostate, liver, breast and lung cancer. By controlling inflammatory mediators, it also exhibits anti-neuroinflammation properties. Hesperidin’s pharmacokinetic profile, including its absorption, stability, and targeted biodistribution, is significantly improved by nano-formulation-driven advances. This eventually improves therapeutic efficiency while reducing side effects linked to conventional treatments. Aim This review constructively explores hesperidin’s pharmacological potential and innovative delivery systems for the treatment of brain disorders, inflammatory conditions, and various cancers. It identifies key knowledge gaps and current limitations, such as poor solubility and impaired absorption, while advocating for advanced nanodelivery systems as promising solutions. By examining the molecular mechanisms underlying hesperidin’s therapeutic effects, we can advance its clinical applications and improve patient outcomes. Materials and methods Literature search was conducted across various databases of Gene Reviews, PubMed, Brain Sciences, ScienceDirect and a search engine Google Scholar to identify potential studies on hesperidin. Published evidence about nano delivery system of hesperidin was included in the review and their therapeutic effect in brain, inflammatory and other associated disorders including cancer. Out of 230 selected 167 literature were finalized to write this manuscript collecting evidence about their formulation, preclinical and clinical findings including 6 patents. This manuscript carries in vitro and in vivo experimental models, facilitating a comparative insight into the molecular pathways engaged. Results Hesperidin demonstrates promising anti-neoplastic, anti-inflammatory effects by effectively regulating inflammatory signalling molecules, potentially responsible for tumour progression. The review comprises of nano-delivery system, that enhance hesperidin’s stability and therapeutic efficacy in preclinical models. Additionally, it underscores the importance of addressing variability in animal models and dosing protocols, which can help refine future research and improve outcomes. Conclusion Hesperidin exhibits anti-inflammatory, anti-carcinogenic, anti-viral, and antioxidant properties, making it a promising phytoconstituent for treating various disorders. However, its low oral bioavailability—caused by poor solubility and limited absorption—poses significant challenges for its therapeutic application in clinical studies. This manuscript aims to inspire researchers to develop alternative strategies and innovative delivery tools to address these challenges, both for preclinical studies and for clinical translation. Graphical abstract This graphical abstract illustrates the diverse therapeutic capabilities of hesperidin, which operates through the modulation of oxidative stress, inflammation, apoptosis, and various metabolic pathways. Its hepatoprotective, neuroprotective, antidiabetic, antiulcer, anticancer, and wound-healing properties are fundamentally supported by the activation of the Nrf2/HO-1 pathway and the inhibition of NF-κB signalling, with further enhancement provided by delivery systems based on nanocarriers. Although hesperidin has promising therapeutic properties, it suffers from low solubility, restricted absorption, and fast metabolism. Sophisticated nanocarrier delivery systems enhance its stability, facilitate controlled release, improve cellular uptake, and increase target specificity, resulting in improved overall therapeutic effectiveness.

Hesperidin: a bioflavonoid with broad therapeutic promise

期刊论文
发表日期：

2026年3月30日

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Sohome Das,
Anuradha Mishra,
Narahari Narayan Palei

摘要

Ethnopharmacological relevance

Hesperidin is a citrus-derived bioflavonoid that has a variety of pharmacological properties, such as anti-inflammatory, anti-carcinogenic, anti-viral and antioxidant properties. It exhibits effectiveness against gastric, colon, prostate, liver, breast and lung cancer. By controlling inflammatory mediators, it also exhibits anti-neuroinflammation properties. Hesperidin’s pharmacokinetic profile, including its absorption, stability, and targeted biodistribution, is significantly improved by nano-formulation-driven advances. This eventually improves therapeutic efficiency while reducing side effects linked to conventional treatments.

Aim

This review constructively explores hesperidin’s pharmacological potential and innovative delivery systems for the treatment of brain disorders, inflammatory conditions, and various cancers. It identifies key knowledge gaps and current limitations, such as poor solubility and impaired absorption, while advocating for advanced nanodelivery systems as promising solutions. By examining the molecular mechanisms underlying hesperidin’s therapeutic effects, we can advance its clinical applications and improve patient outcomes.

Materials and methods

Literature search was conducted across various databases of Gene Reviews, PubMed, Brain Sciences, ScienceDirect and a search engine Google Scholar to identify potential studies on hesperidin. Published evidence about nano delivery system of hesperidin was included in the review and their therapeutic effect in brain, inflammatory and other associated disorders including cancer. Out of 230 selected 167 literature were finalized to write this manuscript collecting evidence about their formulation, preclinical and clinical findings including 6 patents. This manuscript carries in vitro and in vivo experimental models, facilitating a comparative insight into the molecular pathways engaged.

Results

Hesperidin demonstrates promising anti-neoplastic, anti-inflammatory effects by effectively regulating inflammatory signalling molecules, potentially responsible for tumour progression. The review comprises of nano-delivery system, that enhance hesperidin’s stability and therapeutic efficacy in preclinical models. Additionally, it underscores the importance of addressing variability in animal models and dosing protocols, which can help refine future research and improve outcomes.

Conclusion

Hesperidin exhibits anti-inflammatory, anti-carcinogenic, anti-viral, and antioxidant properties, making it a promising phytoconstituent for treating various disorders. However, its low oral bioavailability—caused by poor solubility and limited absorption—poses significant challenges for its therapeutic application in clinical studies. This manuscript aims to inspire researchers to develop alternative strategies and innovative delivery tools to address these challenges, both for preclinical studies and for clinical translation.

Graphical abstract

This graphical abstract illustrates the diverse therapeutic capabilities of hesperidin, which operates through the modulation of oxidative stress, inflammation, apoptosis, and various metabolic pathways. Its hepatoprotective, neuroprotective, antidiabetic, antiulcer, anticancer, and wound-healing properties are fundamentally supported by the activation of the Nrf2/HO-1 pathway and the inhibition of NF-κB signalling, with further enhancement provided by delivery systems based on nanocarriers. Although hesperidin has promising therapeutic properties, it suffers from low solubility, restricted absorption, and fast metabolism. Sophisticated nanocarrier delivery systems enhance its stability, facilitate controlled release, improve cellular uptake, and increase target specificity, resulting in improved overall therapeutic effectiveness.