Enhanced chemotherapeutic efficacy of apigenin liposomes in colorectal cancer based on flavone-membrane interactions

J Colloid Interface Sci. 2017 Apr 1:491:98-110. doi: 10.1016/j.jcis.2016.12.025. Epub 2016 Dec 18.


Recent endeavors in exploiting vast array of natural phytochemicals to ameliorate colorectal cancer led us to investigate apigenin, a naturally occurring dietary flavone as a potential chemo-therapeutic agent. The present study focuses on establishing apigenin as a potential chemotherapeutic agent for alleviating colorectal cancer and reports the development of a stable liposomal nanocarrier with high encapsulation of the hydrophobic flavone apigenin for enhanced chemotherapeutic effects. The enhanced pharmacological activity of apigenin has been assigned to its ability to interact and subsequently influence membrane properties which also resulted in optimal yield of a stable, rigidified, non-leaky nano-carrier with ideal release kinetics. Extensive testing of drug and its liposomal counterpart for potential clinical chemotherapeutic applications yielded hemocompatibility and cytocompatibility with normal fibroblast cells while enhanced antineoplastic activity was observed in tumor xenograft model. The increased chemotherapeutic potential of liposomal apigenin highlights the clinical potential of apigenin-based vesicles.

Keywords: Apigenin; Apoptosis; Cellular arrest; Drug delivery; Liposomes; Membrane.

MeSH terms

  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / chemistry
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Apigenin / chemistry
  • Apigenin / therapeutic use*
  • Cell Cycle / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Colorectal Neoplasms / drug therapy*
  • Colorectal Neoplasms / pathology
  • Drug Screening Assays, Antitumor
  • Flavones / chemistry
  • Flavones / therapeutic use*
  • Humans
  • Liposomes / chemistry
  • Liposomes / therapeutic use
  • Mice
  • Mice, Nude
  • NIH 3T3 Cells
  • Neoplasms, Experimental / drug therapy
  • Neoplasms, Experimental / pathology
  • Particle Size
  • Surface Properties


  • Flavones
  • Liposomes
  • Apigenin