Abstract
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.
Highlights
According to the World Health Organization (WHO), cancer caused around 9.6 million deaths in 2018 and is a leading cause of global fatality [1]
SMV was formulated in chitosan MPs in the present study
Particle size (172 ± 28 μm), with a smooth surface that showed the entrapment of SMV-Chitosan MPs
Summary
According to the World Health Organization (WHO), cancer caused around 9.6 million deaths in 2018 and is a leading cause of global fatality [1]. The recent drug formulations proposed for the cure of this specific kind of cancer have displayed several side effects [3]. For this reason, the introduction of drug delivery systems which can increase the concentrations of a selected drug at the vicinity of target cancer cells is urgently needed. Chitosan-based microparticles (MPs) formulations can release several anti-tumor agents that increase drug internalization into targeted cells and enhance therapeutic effects paralleled by reduced adverse effects [6,7,8]. The term “Eudragit” covers a wide range of non-biodegradable, non-absorbable, and non-toxic polymethacrylate-based copolymers, including neutral as well as charged (anionic and cationic) copolymers prepared by the polymerization of acrylic and methacrylic acids or their esters
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