Preparation of mucoadhesive methacrylated chitosan nanoparticles for delivery of ciprofloxacin

Mucoadhesive polymers and their nanoparticles have attracted a lot of attention in pharmaceutical applications, especially transmucosal drug delivery (TDD). Mucoadhesive polysaccharide-based nanoparticles, particularly chitosan, and its derivatives, are widely used for TDD owing to their outstanding features such as biocompatibility, mucoadhesive, and absorption-enhancing properties. Herein, this study aimed to design potential mucoadhesive nanoparticles for the delivery of ciprofloxacin based on methacrylated chitosan (MeCHI) using the ionic gelation method in the presence of sodium tripolyphosphate (TPP) and compared them with the unmodified chitosan nanoparticles. In this study, different experimental conditions including the polymer to TPP mass ratios, NaCl, and TPP concentration were changed to achieve unmodified and MeCHI nanoparticles with the smallest particle size and lowest polydispersity index. At 4:1 polymer /TPP mass ratio, both chitosan and MeCHI nanoparticles had the smallest size (133 ± 5 nm and 206 ± 9 nm, respectively).

Highlights

Methacrylated chitosan (MeCHI) nanoparticles can be prepared using the ionic gelation method.

Formulation components have significant effects on the properties of MeCHI nanoparticles.

MeCHI nanoparticles provide sustained release of ciprofloxacin.

Ciprofloxacin-loaded MeCHI nanoparticles are more mucoadhesive than their unmodified chitosan counterparts.

MeCHI nanoparticles were generally larger and slightly more polydisperse than the unmodified chitosan nanoparticles. Ciprofloxacin-loaded MeCHI nanoparticles had the highest encapsulation efficiency (69 ± 13 %) at 4:1 MeCHI /TPP mass ratio and 0.5 mg/mL TPP, but similar encapsulation efficiency to that of their chitosan counterpart at 1 mg/mL TPP. They also provided a more sustained and slower drug release compared to their chitosan counterpart. Additionally, the mucoadhesion (retention) study on sheep abomasum mucosa showed that ciprofloxacin-loaded MeCHI nanoparticles with optimized TPP concentration had better retention than the unmodified chitosan counterpart. The percentage of the remained ciprofloxacin-loaded MeCHI and chitosan nanoparticles on the mucosal surface was 96 % and 88 %, respectively. Therefore, MeCHI nanoparticles have an excellent potential for applications in drug delivery.

Renas Rzgar Jalal, Twana Mohammed M. Ways, Mahmoud H. Abu Elella, Diyar Ahmed Hassan, Vitaliy V. Khutoryanskiy, Preparation of mucoadhesive methacrylated chitosan nanoparticles for delivery of ciprofloxacin, International Journal of Biological Macromolecules, Volume 242, Part 4, 2023, 124980, ISSN 0141-8130, https://doi.org/10.1016/j.ijbiomac.2023.124980.

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