Department of Pharmaceutics, College of Pharmacy, University of Sulaimani, Sulaimani 46001, Kurdistan Region, Iraq.
Department of Pharmaceutics, College of Pharmacy, University of Sulaimani, Sulaimani 46001, Kurdistan Region, Iraq.
Int J Biol Macromol. 2023 Jul 1;242(Pt 4):124980. doi: 10.1016/j.ijbiomac.2023.124980. Epub 2023 May 25.
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). 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.
基于甲基丙烯酰化壳聚糖（MeCHI）的潜在黏膜黏附纳米粒的设计及其对环丙沙星的载药传递
黏膜黏附聚合物及其纳米粒在药物传递领域，特别是黏膜给药系统（TDD）中受到了广泛关注。基于黏膜黏附多糖的纳米粒，特别是壳聚糖及其衍生物，由于其生物相容性、黏膜黏附性和吸收增强特性，被广泛应用于 TDD。本研究旨在采用离子凝胶法，以三聚磷酸钠（TPP）为交联剂，设计基于甲基丙烯酰化壳聚糖（MeCHI）的潜在黏膜黏附纳米粒，用于环丙沙星的传递，并将其与未修饰的壳聚糖纳米粒进行比较。本研究通过改变聚合物与 TPP 的质量比、NaCl 和 TPP 浓度等不同实验条件，实现了未修饰和 MeCHI 纳米粒的粒径最小和多分散指数最低。在聚合物/TPP 质量比为 4:1 时，壳聚糖和 MeCHI 纳米粒的粒径最小（分别为 133±5nm 和 206±9nm）。MeCHI 纳米粒通常比未修饰的壳聚糖纳米粒更大，且略微更分散。在 MeCHI/TPP 质量比为 4:1 和 TPP 浓度为 0.5mg/mL 时，载药 MeCHI 纳米粒的包封效率最高（69±13%），但在 TPP 浓度为 1mg/mL 时与壳聚糖纳米粒的包封效率相似。与壳聚糖纳米粒相比，载药 MeCHI 纳米粒具有更持续和更缓慢的药物释放。此外，在绵羊皱胃黏膜上的黏膜黏附（保留）研究表明，具有优化 TPP 浓度的载药 MeCHI 纳米粒在保留方面优于未修饰的壳聚糖纳米粒。载药 MeCHI 和壳聚糖纳米粒在黏膜表面的保留率分别为 96%和 88%。因此，MeCHI 纳米粒在药物传递应用中具有极好的应用潜力。
