Carbohydrate Polymers ( IF 10.7 ) Pub Date : 2022-01-23 , DOI: 10.1016/j.carbpol.2022.119174 Zheng Jin 1 , Gaowei Hu 1 , Kai Zhao 1
There are various challenges for the mucosal delivery of drug, which is largely attributed to the absence of effective drug carriers that can make delivery to mucosal sites. In the present study, we aimed to synthesize bifunctional mucoadhesive nanoparticles (NPs) that could be used for mucosal delivery. N-2-Hydroxypropyl trimethyl ammonium chloride chitosan (M-N-2-HACC) was modified with D-mannose, and N-acetyl-L-cysteine (NAC) was immobilized on the carboxymethyl chitosan (N-CMCS). The electrostatic interaction between the two substances was used to produce mannose-modified thiolated chitosan NPs (M-N-2-HACC/N-CMCS NPs). The NPs showed a particle size of 196.72 ± 0.45 nm and zeta potential of 17.12 ± 0.50 mV. Moreover, it demonstrated high hydrophilicity, enduring drug release, stability, safety, and mucosal adhesion, which contributed to the effectiveness of mucosal administration. Additionally, the NPs could be instantly absorbed by macrophages. Collectively, these results suggested that M-N-2-HACC/N-CMCS NPs could be used as a promising candidate for mucosal delivery.
中文翻译:
甘露糖锚定季铵化壳聚糖/硫醇化羧甲基壳聚糖复合纳米粒子作为药物递送的粘膜粘附载体
药物的粘膜递送存在各种挑战,这在很大程度上归因于缺乏可以将药物递送至粘膜部位的有效药物载体。在本研究中,我们旨在合成可用于粘膜递送的双功能粘膜粘附纳米颗粒 (NPs)。N -2-羟丙基三甲基氯化铵壳聚糖 (MN-2-HACC) 用 D-甘露糖修饰,N-乙酰-L-半胱氨酸(NAC)固定在羧甲基壳聚糖(N-CMCS)上。两种物质之间的静电相互作用被用于生产甘露糖修饰的硫醇化壳聚糖纳米粒子(MN-2-HACC/N-CMCS NPs)。NPs 的粒径为 196.72 ± 0.45 nm,zeta 电位为 17.12 ± 0.50 mV。此外,它表现出高亲水性、持久的药物释放、稳定性、安全性和黏膜粘附性,这有助于黏膜给药的有效性。此外,NPs 可以立即被巨噬细胞吸收。总的来说,这些结果表明 MN-2-HACC/N-CMCS NPs 可用作粘膜递送的有希望的候选者。