Abstract
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.
Highlights
Colon or bowel cancer, known as colorectal cancer (CRC), is the third deadliest type of cancer around the world
The ES 100-coated MPs showed average particle size (200 ± 40 μm), with a smooth surface that demonstrated the entrapment of Ellagic acid (EA)-CHIT-MPs in the eudragit S100 (ES100) MPs matrix (Figure 1B–D)
Glutaraldehyde cross-linking has been developed for stable EA MPs with spherical shape and size of approximately 20(0A±) 40 μm
Summary
Known as colorectal cancer (CRC), is the third deadliest type of cancer around the world. Most of these treatments generate undesired side effects, toxicity, and patient discomfort These adverse effects may be reduced or eliminated via targeted drug delivery. This provides many benefits compared with conventional drug delivery medicines such as increased drug efficiency and stability as well as reduced adverse effects and toxicity Because of their safety and effectiveness, natural products are gaining more attention toward their utilization in cancer chemotherapy [7]. The use of CHIT as a natural carrier of controlled release drugs was previously reported [28,29]. This is due to its improved cost effectiveness, biocompatibility, bioavailability, biodegradability, and reduced toxicity. The use of CHIT as a drug carrier grants increased residence time in the gastrointestinal (GI) tract through mucoadhesion as well as improved cellular permeability [31]
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