Formulation and Physicochemical Characterization of Chitosan-Coated Simvastatin Nanoparticles
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Abstract
Simvastatin is an effective antihyperlipidemic agent whose clinical utility is limited by poor aqueous solubility, low gastrointestinal absorption, and extensive first-pass metabolism, resulting in reduced oral bioavailability. This study aimed to formulate and characterize chitosan-coated simvastatin nanoparticles as a strategy to improve its physicochemical performance and controlled release properties. Nanoparticles were prepared using the ionic gelation method involving electrostatic interaction between chitosan and sodium tripolyphosphate. The developed formulation was evaluated by in vitro drug release studies, scanning electron microscopy (SEM), and Fourier transform infrared spectroscopy (FTIR). The release profile demonstrated a biphasic pattern with an initial burst release during the early phase, followed by sustained drug release reaching approximately 70–75% over 300 minutes, indicating effective controlled-release behavior. SEM analysis showed clear morphological transformation from loosely aggregated crystalline simvastatin particles to denser and more cohesive nanoparticulate structures after chitosan coating, confirming successful encapsulation. FTIR spectra retained the characteristic peaks of both simvastatin and chitosan with only minor shifts in band positions, suggesting structural integrity of the drug and absence of significant chemical incompatibility between formulation components. The combined findings indicate that chitosan coating improved the physicochemical characteristics of simvastatin while providing sustained release potential. Therefore, chitosan-coated simvastatin nanoparticles represent a promising oral nanocarrier system for enhancing simvastatin delivery and therapeutic performance
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References
Crucho, C. I. C., & Barros, M. T. (2017). Polymeric nanoparticles: A study on the preparation variables and characterization methods. Materials Science and Engineering: C, 80, 771–784. https://doi.org/10.1016/j.msec.2017.06.004
Chinaeke, E. E., Chime, S. A., Kenechukwu, F. C., Müller-Goymann, C. C., Attama, A. A., & Okore, V. C. (2014). Formulation of novel artesunate-loaded solid lipid microparticles (SLMs) based on dika wax matrices: In vitro and in vivo evaluation. Journal of Drug Delivery Science and Technology, 24(1), 69–77.
Faris, T. M., Harisa, G. I., Alanazi, F. K., Samy, A. M., & Nasr, F. A. (2020). Developed simvastatin chitosan nanoparticles co-crosslinked with tripolyphosphate and chondroitin sulfate for ASGPR-mediated targeted HCC delivery with enhanced oral bioavailability. Saudi Pharmaceutical Journal, 28(12), 1851–1867. https://doi.org/10.1016/j.jsps.2020.11.012
George, M., & Ghosh, I. (2013). Identifying the correlation between drug/stabilizer properties and critical quality attributes (CQAs) of nanosuspension formulation prepared by wet milling technology. European Journal of Pharmaceutical Sciences, 48(1–2), 142–152.
Harisa, G. I., Badran, M. M., Attia, S. M., Alanazi, F. K., & Shazly, G. A. (2018). Influence of pravastatin chitosan nanoparticles on erythrocytes cholesterol and redox homeostasis: An in vitro study. Arabian Journal of Chemistry, 11(8), 1236–1246. https://doi.org/10.1016/j.arabjc.2015.02.008
Kim, D., Jeong, Y., Choi, C., Roh, S., Kang, S., Jang, M., et al. (2006). Retinol-encapsulated low molecular water-soluble chitosan nanoparticles. International Journal of Pharmaceutics, 319, 130–138.
Kongsong, M., Songsurang, K., Sangvanich, P., & Sirilertmukul, K. (2014). Design, synthesis, fabrication and in vitro evaluation of mucoadhesive 5-amino-2-mercaptobenzimidazole chitosan as low water soluble drug carriers. European Journal of Pharmaceutics and Biopharmaceutics. https://doi.org/10.1016/j.ejpb.2014.08.016
Nilay, K. (2019). Water soluble chitosan derivatives and their biological activities: A review. Polymer Sciences, 5(1), 3.
Sarathchandiran, I., Koumaravelou, K., & Selvasudha, N. (2019). Interaction pattern and in vitro, in vivo release behavior of simvastatin-loaded chitosan nanoformulation. Drug Development and Industrial Pharmacy, 45(11), 1725–1739. https://doi.org/10.1080/03639045.2019.1656737
Selvasudha, N., Koumaravelou, K., & Sri Durgadevi, N. (2017). Optimization of formulation parameters and characterization of simvastatin loaded chitosan nanoparticles. International Journal of Advanced Research, 5(2), 2386–2400. https://doi.org/10.21474/IJAR01/3422
Selvasudha, N., & Koumaravelou, K. (2017). The multifunctional synergistic effect of chitosan on simvastatin loaded nanoparticulate drug delivery system. Carbohydrate Polymers, 163, 70–80. https://doi.org/10.1016/j.carbpol.2017.01.069
Severino, P., da Silva, C. F., da Silva, M. A., Santana, M. H. A., & Souto, E. B. (2016). Chitosan cross-linked pentasodium tripolyphosphate micro/nanoparticles produced by ionotropic gelation. Sugar Tech, 18(1), 49–54. https://doi.org/10.1007/s12355-014-0360-z
Shavi, G. V., Nayak, U. Y., Reddy, M. S., Karthik, A., Deshpande, P. B., Kumar, A. R., & Udupa, N. (2011). Sustained release optimized formulation of anastrozole-loaded chitosan microspheres: In vitro and in vivo evaluation. Journal of Materials Science: Materials in Medicine, 22(4), 865–878. https://doi.org/10.1007/s10856-011-4274-y
Shinde, A. J., & Harinath, N. (2014). Formulation, development and characterization of simvastatin nanoparticles by solvent displacement method. Der Pharmacia Lettre, 6(2), 145–155.
Tulbah, A. S., Pisano, E., Landh, E., Scalia, S., & Young, et al. (2019). Simvastatin nanoparticles reduce inflammation in LPS-stimulated alveolar macrophages. Journal of Pharmaceutical Sciences, 1–22. https://doi.org/10.1016/j.xphs.2019.08.029
Ullah, F., Khan, M. F. A., Khan, N. H., Rehman, M. F., Shah, S. S., Mustaqeem, M., Khan, A. S., Khan, S., & Shi, H. (2022). Simvastatin-loaded lipid emulsion nanoparticles: Characterizations and applications. ACS Omega, 7(27), 23643–23652. https://doi.org/10.1021/acsomega.2c02153
Valo, H., Arola, S., Laaksonen, P., Torkkeli, M., Peltonen, L., Linder, M. B., Serimaa, R., Kuga, S., Hirvonen, J., & Laaksonen, T. (2013). Drug release from nanoparticles embedded in four different nanofibrillar cellulose aerogels. European Journal of Pharmaceutics and Biopharmaceutics, 50, 69–77