Therapeutic applications of apigenin and its derivatives: micro and nano aspects

Document Type : Mini-Review


1 Department of Neuroscience and Addiction Studies, School of Advanced Technologies in Medicine, Tehran University of Medical Sciences, Tehran, Iran

2 Department of Biology, Faculty of Science, Khorramabad, Lorestan University, Lorestan, Iran

3 Department of Biology, Faculty of Science, Razi University, Kermanshah, Iran



Antibacterial, antifungal, antiviral, antiparasitic, antioxidant, antiangiogenic, antitumor, antidiabetic, antihyperlipidemic, and antineurodegenerative properties have been indicated for various types of flavonoids and their derivatives. Apigenin as a flavonoid metabolite, a flavone, from the genus Apium related to the flavone class can be found in many plant species including Petroselinum crispum, Apium graveolens, and Matricaria recutita. Lower bioavailability and specificity are two main barriers to obtaining effective formulations. Application of micro and nanoformulations based on organic and inorganic materials can improve the bioavailability and specificity of apigenin and its derivatives such as apigenin 7-O-beta-d-glucoside, apigenin 7-glucoside-4’-trans-caffeate, and apigenin 7-glucoside-4’-p-coumarate. However, there are various limitations to getting suitable formulations in physiological conditions. In this regard, this review has addressed these issues according to recent studies.

Graphical Abstract

Therapeutic applications of apigenin and its derivatives: micro and nano aspects


  • Low solubility and bioavailability are two main limitations of the formulation of apigenin for therapeutic aspects.
  • Micro and nanoformulations including micelles, liposomes, SLN, NLC, cubosomes, niosomes, phytosomes, and bilosomes may optimize the bioavailability of apigenin inside the body.
  • Apigenin can form antimicrobial multifunctional benzoxazine by reacting with formaldehyde and furfurylamine/stearylamine.
  • In the case of Parkinson’s mouse model, apigenin administration reversed the changes in expressions and concentrations of TNF-α, IL-1β, IL-6, IL-10, and TGF-β in brain tissue.


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