Chitosan coated microparticles enhance simvastatin colon targeting and pro-apoptotic activity

Nabil A. Alhakamy, Usama A. Fahmy, Osama A.A. Ahmed, Giuseppe Caruso, Filippo Caraci, Hani Z. Asfour, Muhammed A. Bakhrebah, Mohammad N. Alomary, Wesam H. Abdulaal, Solomon Z. Okbazghi, Ashraf B. Abdel-Naim, Basma G. Eid, Hibah M. Aldawsari, Mallesh Kurakula, Amir I. Mohamed

Research output: Contribution to journalArticlepeer-review


This work aimed at improving the targeting and cytotoxicity of simvastatin (SMV) against colon cancer cells. SMV was encapsulated in chitosan polymers, followed by eudragit S100 microparticles. The release of SMV double coated microparticles was dependent on time and pH. At pH 7.4 maximum release was observed for 6 h. The efficiency of the double coat to target colonic tissues was confirmed using real-time X-ray radiography of iohexol dye. Entrapment efficiency and particle size were used in the characterization of the formula. Cytotoxicity of SMV microparticles against HCT-116 colon cancer cells was significantly improved as compared to raw SMV. Cell cycle analysis by flow cytomeric technique indicated enhanced accumulation of colon cancer cells in the G2/M phase. Additionally, a significantly higher cell fraction was observed in the pre-G phase, which highlighted enhancement of the proapoptotic activity of SMV prepared in the double coat formula. Assessment of annexin V staining was used for confirmation. Cell fraction in early, late and total cell death were significantly elevated. This was accompanied by a significant elevation of cellular caspase 3 activity. In conclusion, SMV-loaded chitosan coated with eudragit S100 formula exhibited improved colon targeting and enhanced cytotoxicity and proapoptotic activity against HCT-116 colon cancer cells.

Original languageEnglish
Article number226
JournalMarine Drugs
Issue number4
Publication statusPublished - Apr 2020


  • Chitosan
  • Drug release
  • Microparticles
  • Mucoadhesion
  • Simvastatin

ASJC Scopus subject areas

  • Drug Discovery


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