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Ureido-modified carboxymethyl chitosan-graft-stearic acid polymeric nano-micelles as a targeted delivering carrier of clarithromycin for Helicobacter pylori: Preparation and in vitro evaluation
- Cong, Ying, Geng, Jiayue, Wang, Hongying, Su, Jing, Arif, Muhammad, Dong, Quanjiang, Chi, Zhe, Liu, Chenguang
- International journal of biological macromolecules 2019 v.129 pp. 686-692
- Helicobacter pylori, bioavailability, chitosan, clarithromycin, composite polymers, cytotoxicity, drugs, gastric juice, in vitro studies, mucus, particle size, stearic acid, stomach, urea
- The effect of antibiotics in the stomach for curing Helicobacter pylori infection is hampered by the adverse gastric environment and low bioavailability of the administered drugs. Concerning these challenges, a polymeric nano-micelle was developed. Initially, carboxymethyl chitosan (CMCS) was hydrophobically modified with stearic acid (SA), and the obtained CMCS-g-SA co-polymers was further conjugated with urea to acquire U-CMCS-g-SA co-polymers. Sphere-shaped nano-micelles (UCS-NMs) with the particle sizes of approximately 200nm were obtained with the U-CMCS-g-SA co-polymers. It was specified that this nano-micelle had no cell toxicity to AGS cells, and it could maintain a stable particle size for 6h in simulated gastric fluid and for 24h in 1×PBS. Attractively, the CMCS backbones granted this nano-micelle an excellent retention time in the stomach, almost 24h; meanwhile, the grafted ureido groups conferred effective targeting to H. pylori. This nano-micelle could load clarithromycin with high efficiency and exhibited slow release of this antibiotic in a slightly alkaline environment. In vitro inhibitory assay also indicated that a significantly enhanced anti-H. pylori activity was achieved by using this nano-micelle. This work demonstrated that the U-CMCS-g-SA nano-micelle is a proper carrier for targeted delivery of clarithromycin to H. pylori under the gastric mucus layer.