Micro and nano formulas of phyto-drugs naringenin and naringin with antineoplastic activity: Cellular and molecular aspects

Document Type : Narrative Review


1 Department of Plant Production and Genetics, Faculty of Agriculture, Razi University, Kermanshah, Iran

2 Department of Bacteriology, Faculty of Medical Sciences, Tarbiat Modares University, Tehran,Iran

3 School of Science and Engineering, Duquesne University, Pittsburgh, USA



Drug resistance and metastasis process are two well-known hindrances to the eradication of cancer cells. Naringin and naringenin flavonoids have anticancer activities against various types of tumors. The inhibition of several cell signal transduction pathways has been found for combination therapy composed of naringin and naringenin. Naringin has a larger molecular volume with higher flexibility compound than naringenin. Low water solubility and unsuitable bioavailability are the main disadvantages of these phytocompounds. Tremendous efforts are needed for the transition of the bioactive compounds of hydrophobic naringenin and nanringin from preclinical to clinical application. Increasing the half-life of naringenin and naringin in blood circulation is the critical factor for obtaining maximum therapeutic outcomes in physiological conditions. Polymeric and lipid nanocarriers have illustrated unique properties compared to conventional drug delivery systems. This review compared the efficacy of these novel carriers for the loading and encapsulation of naringin and naringenin metabolites.

Graphical Abstract

Micro and nano formulas of phyto-drugs naringenin and naringin with antineoplastic activity: Cellular and molecular aspects


  • Naringin compared to naringenin shows different values for a given conformation-dependent physicochemical property.
  • Low bioavailability of naringin and naringenin can hinder the transition of these natural compounds from preclinical to clinical application.
  • Co-delivery of naringin with paclitaxel showed synergistic anti-neoplastic activity against breast cancer cells.
  • Induction of apoptosis in cancer cells can be caused by naringin-dextrin nanoformulation.
  • The prolonged release of anticancer agents in the tumor environment is a critical factor in maximizing therapeutic results.
  • Naringenin-CNTs exhibited sustained release of naringenin in pH 5.5.


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