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Chitosan coated microparticles enhance simvastatin colon targeting and pro-apoptotic activity
- Source :
- Marine Drugs, Volume 18, Issue 4, Marine Drugs, Vol 18, Iss 226, p 226 (2020)
- Publication Year :
- 2020
-
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.
- Subjects :
- Male
Simvastatin
Colorectal cancer
Pharmaceutical Science
Antineoplastic Agents
Apoptosis
02 engineering and technology
Mucoadhesion
Microparticles
Article
Chitosan
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
Drug Delivery Systems
Polymethacrylic Acids
Annexin
Drug Discovery
medicine
Animals
Humans
Particle Size
Cytotoxicity
Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
lcsh:QH301-705.5
Drug Carriers
Chemistry
Drug release
Hydrogen-Ion Concentration
021001 nanoscience & nanotechnology
medicine.disease
HCT116 Cells
Molecular biology
Microspheres
Staining
lcsh:Biology (General)
030220 oncology & carcinogenesis
Colonic Neoplasms
Rabbits
0210 nano-technology
medicine.drug
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Journal :
- Marine Drugs, Volume 18, Issue 4, Marine Drugs, Vol 18, Iss 226, p 226 (2020)
- Accession number :
- edsair.doi.dedup.....9bb5450d5c38bf15841c8365ec26344a