Comparative Release Kinetics and Mechanistic Modeling of Mesalazine from PEGylated Chitosan-Coated Niosomes

Authors

https://doi.org/10.48313/bic.vi.68

Abstract

Mesalazine is widely used in the treatment of Inflammatory Bowel Diseases (IBD); however, its therapeutic efficacy may be limited by rapid drug release and insufficient retention at the target site. In the present study, PEGylated chitosan-coated niosomes (PEG-CS-MEZ-NIO) were developed as a controlled-release delivery system for mesalazine. The formulation was prepared using the thin-film hydration method followed by chitosan surface modification. Encapsulation efficiency, permeability, in vitro drug release behavior, and release kinetics were investigated. The prepared formulation exhibited a high encapsulation efficiency of 95.42%, indicating effective drug entrapment within the vesicular structure. Permeability studies demonstrated excellent storage stability with minimal drug leakage under refrigerated conditions. In vitro release studies revealed a biphasic release profile characterized by an initial burst release followed by a sustained release phase, reaching a cumulative release of 29.8% after 270 min. To elucidate the release mechanism, the experimental data were fitted to zero-order, first-order, Higuchi, and Korsmeyer-Peppas kinetic models. Among the investigated models, the Higuchi model provided the highest correlation coefficient (R²=0.9990), suggesting diffusion-controlled release as the predominant mechanism. Furthermore, the Korsmeyer-Peppas model yielded a release exponent of n=0.8852, indicating anomalous (non-Fickian) transport involving both diffusion and polymer relaxation processes. The findings demonstrate that PEGylated chitosan-coated niosomes can effectively regulate mesalazine release and represent a promising platform for sustained drug delivery applications.

Keywords:

Mesalazine, Niosomes, PEGylation, Release kinetics, Higuchi model, Drug delivery system

References

  1. [1] Camilleri, M. (2015). Guanylate cyclase C agonists: Emerging gastrointestinal therapies and actions. Gastroenterology, 148(3), 483–487. https://www.gastrojournal.org/article/S0016-5085(15)00015-3/fulltext
  2. [2] Saraswathi, T. S., Mothilal, M., & Jaganathan, M. K. (2019). Niosomes as an emerging formulation tool for drug delivery-a review. International journal of applied pharmaceutics, 11(2), 7–15. https://doi.org/10.22159/ijap.2019v11i2.30534
  3. [3] Kahn, S. E., Hull, R. L., & Utzschneider, K. M. (2006). Mechanisms linking obesity to insulin resistance and type 2 diabetes. Nature, 444(7121), 840–846. https://www.nature.com/articles/nature05482
  4. [4] Diamanti-Kandarakis, E., Christakou, C. D., Kandaraki, E., & Economou, F. N. (2010). Metformin: An old medication of new fashion: Evolving new molecular mechanisms and clinical implications in polycystic ovary syndrome. European journal of endocrinology, 162(2), 193–212. https://doi.org/10.1530/EJE-09-0733
  5. [5] De Lima, J. G., & Nóbrega, L. H. C. (2013). Oral therapies for type 2 diabetes. In Endocrinology and diabetes: A problem-oriented approach (pp. 375–384). Springer. https://doi.org/10.1007/978-1-4614-8684-8_29
  6. [6] Baniasad, A., Baei, M. S., & Tala-Tapeh, S. M. (2025). Chitosan-PEGylated niosomes and liposomes as biomacromolecule carriers for Alzheimer’s disease treatment: Galantamine drug delivery carrier. Materials chemistry and physics, 352, 132003. https://doi.org/10.1016/j.matchemphys.2025.132003
  7. [7] Sharma, H. K., Lahkar, S., & Nath, L. K. (2013). Formulation and in vitro evaluation of metformin hydrochloride loaded microspheres prepared with polysaccharide extracted from natural sources. Acta pharmaceutica, 63(2), 209–222. https://doi.org/10.2478/acph-2013-0019
  8. [8] Sharma, A., & Sharma, U. S. (1997). Liposomes in drug delivery: Progress and limitations. International journal of pharmaceutics, 154(2), 123–140. https://doi.org/10.1016/S0378-5173(97)00135-X
  9. [9] Chandrasekhar, P., & Kaliyaperumal, R. (2026). Development of transfersomal buccal patches of galantamine for enhanced bioavailability in Alzheimer’s disease therapy. Journal of applied pharmaceutical research, 14(2), 61–75. https://doi.org/10.69857/joapr.v14i2.1523
  10. [10] Ashtikar, M., Nagarsekar, K., & Fahr, A. (2016). Transdermal delivery from liposomal formulations-evolution of the technology over the last three decades. Journal of controlled release, 242, 126–140. https://doi.org/10.1016/j.jconrel.2016.09.008
  11. [11] Yusaf, R., Nawaz, R., Hayat, S., Khursheed, A., Zafar, N., Ahmad, A., … & Majeed, I. (2014). Structural components of liposomes and characterization tools. American journal of pharm research, 4(08), 3559–3567. https://b2n.ir/ry9505
  12. [12] Lu, Q., Lu, P. M., Piao, J. H., Xu, X. L., Chen, J., Zhu, L., & Jiang, J. G. (2014). Preparation and physicochemical characteristics of an allicin nanoliposome and its release behavior. LWT-food science and technology, 57(2), 686–695. https://doi.org/10.1016/j.lwt.2014.01.044
  13. [13] Pulak Das, P. D., Santosh Joshi, S. J., Jayashree Rout, J. R., & Upreti, D. K. (2013). Lichen diversity for environmental stress study: Application of index of atmospheric purity (IAP) and mapping around a paper mill in Barak Valley, Assam, Northeast India. Tropical ecology, 54(3), 355–364. https://www.cabidigitallibrary.org/doi/full/10.5555/20133376775
  14. [14] Wilczewska, A. Z., Niemirowicz, K., Markiewicz, K. H., & Car, H. (2012). Nanoparticles as drug delivery systems. Pharmacological reports, 64(5), 1020–1037. https://doi.org/10.1016/S1734-1140(12)70901-5
  15. [15] Patel, A., Ray, S., & Thakur, R. S. (2006). Invitro evaluation and optimization of controlled release floating drug delivery system of metformin hydrochloride. DARU journal of pharmaceutical sciences, 14(2), 57–64. https://daru.tums.ac.ir/index.php/daru/article/view/265
  16. [16] Georgieva, D., Nikolova, D., Vassileva, E., & Kostova, B. (2023). Chitosan-based nanoparticles for targeted nasal galantamine delivery as a promising tool in Alzheimer’s disease therapy. Pharmaceutics, 15(3), 829. https://doi.org/10.3390/pharmaceutics15030829
  17. [17] Kushnazarova, R., Mirgorodskaya, A., Lenina, O., Petrov, K., Lyubina, A., Voloshina, A., … & Zakharova, L. (2025). Niosomes and tocosomes as promising nanocontainers for the antidiabetic drug repaglinide. Materials today chemistry, 50, 103223. https://doi.org/10.1016/j.mtchem.2025.103223
  18. [18] Dogra, S. (2011). A chitosan-polymer hydrogel bead system for a metformin hydrochloride controlled release oral dosage form [Thesis]. https://www.proquest.com/openview/a11b28655d5f0365efbfc5c7a5ab5c41/1?pq-origsite=gscholar&cbl=18750
  19. [19] Banerjee, P., Deb, J., Roy, A., Ghosh, A., & Chakraborty, P. (2012). Fabrication and development of pectin microsphere of metformin hydrochloride. International scholarly research notices, 2012(1), 230621. https://doi.org/10.5402/2012/230621
  20. [20] Pradeep, A. R., Nagpal, K., Karvekar, S., Patnaik, K., Naik, S. B., & Guruprasad, C. N. (2015). Platelet-rich fibrin with 1% metformin for the treatment of intrabony defects in chronic periodontitis: A randomized controlled clinical trial. Journal of periodontology, 86(6), 729–737. https://doi.org/10.1902/jop.2015.140646
  21. [21] Marzban, A., Akbarzadeh, A., Ardestani, M. S., Ardestani, F., & Akbari, M. (2018). Synthesis of nano-niosomal deferoxamine and evaluation of its functional characteristics to apply as an iron-chelating agent. The canadian journal of chemical engineering, 96(1), 107–112. https://doi.org/10.1002/cjce.23048
  22. [22] Xia, F., Hu, D., Jin, H., Zhao, Y., & Liang, J. (2012). Preparation of lutein proliposomes by supercritical anti-solvent technique. Food hydrocolloids, 26(2), 456–463. https://doi.org/10.1016/j.foodhyd.2010.11.014
  23. [23] Kester, M., El-Bayoumy, K., Skibinski, C., & Das, A. (2019). Acid stable liposomal compositions and methods for producing the same. The Penn State Research Foundation. https://patents.google.com/patent/US10272041B2/en

Downloads

Published

2026-09-28

Issue

Vol. 3 No. 2 (2026): Biocompounds

Section

Articles

How to Cite

Abdolmaleki, E. . . (2026). Comparative Release Kinetics and Mechanistic Modeling of Mesalazine from PEGylated Chitosan-Coated Niosomes. Biocompounds, 3(2), 96–105. https://doi.org/10.48313/bic.vi.68

Similar Articles

11-19 of 19

You may also start an advanced similarity search for this article.