RETRACTED: Chitosan-Based Microparticles Enhance Ellagic Acid’s Colon Targeting and Proapoptotic Activity

Abstract

<jats:p>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.</jats:p>

Chebulinic acid inhibits MDA‐MB‐231 breast cancer metastasis and promotes cell death through down regulation of SOD1 and induction of autophagy

“…Chebulagic acid has been shown to have significant anti angiogenic (Athira et al, 2017) and antitumor activity against colorectal carcinoma and retinoblastoma cell lines (Kumar, Gangappa, Gupta, & Karnati, 2014; Reddy et al, 2009). Similarly, it has been demonstrated that ellagic acid can induce apoptosis in breast, prostrate, colon, and lung cancer cells (Alhakamy et al, 2020, Duan et al, 2020; Mohammed Saleem and Selim, 2020; Yousuf et al, 2020). Gallic acid, another polyphenol present in Triphala preparation also demonstrates significant anticancer and apoptotic activity (Alfei, Marengo, Zuccari, Turrini, & Domenicotti, 2020; Jang, Ko, & Choi, 2020; Patra et al, 2020, Priyadarshi et al, 2020).…”

Novel Approaches to Enhance Oral Bioavailability of Poorly Soluble Drugs

“…Several conventional methods like Co-solvency and surfactant solubilisation; pH modification, microparticles [6,7] and salt forms; Cyclodextrins (CDs); solid state modification including, amorphous forms, solid dispersions and co-crystals etc. CDs (Inclusion complexation) are the are the multipurpose excipients studied widely for pharmaceutical purposes.…”

Clinical implications of novel polymer and lipid based drug delivery systems

“…Biodegradable and bio reducible polymers have made possible a choice for many new drug delivery systems. [30] For polymer-based drug delivery systems natural polymers such as polysaccharides, dextrin, chitosan (obtained from shellfish) [31] , arginine, alginate (derived from brown seaweed known as Phaeophyceae), Zein (found in corn) and hyaluronic acid are used. Synthetic polymers such as dendrite polymers, 2-hydroxyethyl methacrylate, PLGA (elastomeric copolymer) and Nisopropyl acrylamide are used.…”