Chitosan-based microparticles enhance ellagic acid’s colon targeting and proapoptotic activity

Nabil A. Alhakamy, Osama A.A. Ahmed, Mallesh Kurakula, Giuseppe Caruso, Filippo Caraci, Hani Z. Asfour, Anas Alfarsi, Basma G. Eid, Amir I. Mohamed, Nabil K. Alruwaili, Wesam H. Abdulaal, Usama A. Fahmy, Hani A. Alhadrami, Basmah M. Eldakhakhny, Ashraf B. Abdel-Naim

Research output: Contribution to journalArticlepeer-review


This study aimed at improving the targeting and cytotoxic effect of ellagic acid (EA) on colon cancer cells. EA was encapsulated in chitosan (CHIT) polymers then coated by eudragit S100 (ES100) microparticles. The release of EA double-coated microparticles (MPs) was tested at simulative pH values. Maximum release was observed at 24 h and pH 7.4. The cytotoxicity of EA MPs on HCT 116 colon cancer cells was synergistically improved as compared with raw EA. Cell-cycle analysis by flow cytometry suggested enhanced G2-M phase colon cancer cell accumulation. In addition, a significantly higher cell fraction was observed in the pre-G phase, which highlighted the enhancement of the proapoptotic activity of EA formulated in the double-coat mixture. Annexin-V staining was used for substantiation of the observed cell-death-inducing activity. Cell fractions were significantly increased in early, late, and total cell death. This was backed by high elevation in cellular content of caspase 3. Effectiveness of the double-coated EA to target colonic tissues was confirmed using real-time iohexol dye X-ray radiography. In conclusion, CHIT loaded with EA and coated with ES100 formula exhibits improved colon targeting as well as enhanced cytotoxic and proapoptotic activity against HCT 116 colon cancer when compared with the administration of raw EA.

Original languageEnglish
Article number652
Pages (from-to)1-14
Number of pages14
Issue number7
Publication statusPublished - Jul 2020


  • Chitosan
  • Colon targeting
  • Drug release
  • Ellagic acid
  • Muco-adhesion

ASJC Scopus subject areas

  • Pharmaceutical Science


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