Carbohydrate Polymers ( IF 11.2 ) Pub Date : 2020-07-22 , DOI: 10.1016/j.carbpol.2020.116782 Samah Attia Algharib 1 , Ali Dawood 2 , Kaixiang Zhou 3 , Dongmei Chen 4 , Chao Li 3 , Kuiyu Meng 3 , Muhammad Kashif Maa 3 , Saeed Ahmed 3 , Lingli Huang 5 , Shuyu Xie 4
Due to the poor solubility and permeability of rifaximin (RFX), it is not effective against intracellular pathogens although it shows strong activity against most bacteria. To develop an effective mucoadhesive drug delivery system with a targeted release in bacterial infection site, RFX-loaded chitosan (CS)/carboxymethyl-chitosan (CMCS) nanogel was designed and systematically evaluated. FTIR, DSC, and XRD demonstrated that the nanogel was formed by interactions between the positively charged NH3+ on CS and CMCS, and the negatively charged COO on CMCS. RFX was encapsulated into the optimized nanogel in amorphous form. The nanogel was a uniform spherical shape with a mean diameter of 171.07 nm. It had excellent sustained release, strong mucin binding ability, and pH-responsive properties of quicker swelling and release at acidic pH. It showed low hemolytic ratio and high antioxidant activity. The present investigation indicated that the CS-nanogel could be potentially used as a promising bacterial responsiveness drug delivery system.
中文翻译:
利福昔明负载的壳聚糖-羧甲基壳聚糖纳米凝胶的设计,结构测定和生物学效应。
由于利福昔明(RFX)的溶解性和渗透性差,尽管它对大多数细菌表现出强大的活性,但它对细胞内病原体无效。为了开发在细菌感染部位靶向释放的有效粘膜粘附药物递送系统,设计并系统评估了RFX负载的壳聚糖(CS)/羧甲基壳聚糖(CMCS)纳米凝胶。FTIR,DSC和XRD证明纳米凝胶是由带正电的NH 3 +之间的相互作用形成的在CS和CMCS上,以及在CMCS上带负电的COO。RFX以无定形形式封装在优化的纳米凝胶中。纳米凝胶是均匀的球形,平均直径为171.07nm。它具有出色的持续释放,强大的粘蛋白结合能力,以及在酸性pH下具有更快溶胀和释放的pH响应特性。它显示出低溶血率和高抗氧化活性。本研究表明,CS-纳米凝胶可潜在地用作有希望的细菌反应性药物递送系统。