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Article

Chitosan Coated Microparticles Enhance Simvastatin Colon Targeting and Pro-Apoptotic Activity

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Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia
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Center of Excellence for Drug Research and Pharmaceutical Industries, King Abdulaziz University, Jeddah 21589, Saudi Arabia
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King Fahd Medical Research Center, King Abdulaziz University, Jeddah 21589, Saudi Arabia
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Advanced Drug Delivery Research Group, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia
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Oasi Research Institute—IRCCS, Via Conte Ruggero, 73, 94018 Troina (EN), Italy
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Department of Drug Sciences, University of Catania, 95125 Catania, Italy
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Department of Medical Microbiology and Parasitology, Faculty of Medicine, Princess Al-Jawhara Center of Excellence in Research of Hereditary Disorders, King Abdulaziz University, Jeddah 21589, Saudi Arabia
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Life Science and Environment Research Institute, King Abdulaziz City for Science and Technology (KACST), P.O. Box 6086, Riyadh 11442, Saudi Arabia
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Department of Biochemistry, Cancer Metabolism and Epigenetic Unit, Faculty of Science, King Abdulaziz University, Jeddah 21589, Saudi Arabia
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Global Analytical and Pharmaceutical Development, Alexion Pharmaceuticals, New Haven, CT 06510, USA
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Department of Pharmacology and Toxicology, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia
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Department of Biomedical Engineering, University of Memphis, Memphis, TN 38152, USA
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Department of Pharmaceutics and Industrial Pharmacy, Military Medical Academy, Cairo 11435, Egypt
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Author to whom correspondence should be addressed.
Mar. Drugs 2020, 18(4), 226; https://doi.org/10.3390/md18040226
Received: 21 March 2020 / Revised: 13 April 2020 / Accepted: 21 April 2020 / Published: 24 April 2020
(This article belongs to the Special Issue Application of Marine Chitin and Chitosan)
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. View Full-Text
Keywords: chitosan; simvastatin; drug release; microparticles; mucoadhesion chitosan; simvastatin; drug release; microparticles; mucoadhesion
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MDPI and ACS Style

Alhakamy, N.A.; Fahmy, U.A.; Ahmed, O.A.A.; Caruso, G.; Caraci, F.; Asfour, H.Z.; Bakhrebah, M.A.; N. Alomary, M.; Abdulaal, W.H.; Okbazghi, S.Z.; Abdel-Naim, A.B.; Eid, B.G.; Aldawsari, H.M.; Kurakula, M.; Mohamed, A.I. Chitosan Coated Microparticles Enhance Simvastatin Colon Targeting and Pro-Apoptotic Activity. Mar. Drugs 2020, 18, 226. https://doi.org/10.3390/md18040226

AMA Style

Alhakamy NA, Fahmy UA, Ahmed OAA, Caruso G, Caraci F, Asfour HZ, Bakhrebah MA, N. Alomary M, Abdulaal WH, Okbazghi SZ, Abdel-Naim AB, Eid BG, Aldawsari HM, Kurakula M, Mohamed AI. Chitosan Coated Microparticles Enhance Simvastatin Colon Targeting and Pro-Apoptotic Activity. Marine Drugs. 2020; 18(4):226. https://doi.org/10.3390/md18040226

Chicago/Turabian Style

Alhakamy, Nabil A., 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, and Amir I. Mohamed 2020. "Chitosan Coated Microparticles Enhance Simvastatin Colon Targeting and Pro-Apoptotic Activity" Marine Drugs 18, no. 4: 226. https://doi.org/10.3390/md18040226

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