College of Pharmacy, Aljouf University, Sakaka, Saudi Arabia.
Glocal School of Pharmacy, The Glocal University, Saharanpur, Uttar Pradesh, India.
Int J Biol Macromol. 2018 Mar;108:650-659. doi: 10.1016/j.ijbiomac.2017.11.170. Epub 2017 Dec 22.
In this study, chitosan nanoparticles (CH-NPs) were used to encapsulate antibacterial agent levofloxacin for the treatment of ocular infection. The chitosan nanoparticles were prepared by ionic gelation method using chitosan and sodium tripolyphosphate. The developed formulations were evaluated for various physicochemical parameters and optimized formulation was converted into the sol-gel system to enhance the corneal residence time. The developed formulations showed the particle size in nanometric range with high encapsulation, and loading. HET-CAM test and histopathology of cornea demonstrated that optimized formulation was found to be non-irritant and safe for topical ophthalmic use. The antimicrobial study revealed that the developed formulation possesses higher antibacterial activity against P. aeruginosa, and S. aureus. The pharmacoscintigraphic study result revealed the reduced corneal clearance, naso-lachrymal drainage as well as higher retention of LFX in comparison to LFX solution. Our results concluded that levofloxacin loaded chitosan nanoparticles in situ gel system found to be an efficient carrier for ocular delivery of levofloxacin.
在这项研究中,壳聚糖纳米粒子(CH-NPs)被用于封装抗菌剂左氧氟沙星,以治疗眼部感染。壳聚糖纳米粒子是通过壳聚糖和三聚磷酸钠的离子凝胶化方法制备的。所开发的制剂经过各种物理化学参数的评估,并将优化的制剂转化为溶胶-凝胶系统,以延长角膜停留时间。所开发的制剂表现出纳米级的粒径,具有高包封率和载药量。HET-CAM 试验和角膜组织病理学表明,优化的制剂被发现是非刺激性的,可安全用于局部眼科应用。抗菌研究表明,与左氧氟沙星溶液相比,所开发的制剂对铜绿假单胞菌和金黄色葡萄球菌具有更高的抗菌活性。药代动力学研究结果表明,与左氧氟沙星溶液相比,载有左氧氟沙星的壳聚糖纳米粒子原位凝胶系统具有降低的角膜清除率、鼻泪液引流以及更高的左氧氟沙星保留率。我们的研究结果表明,左氧氟沙星负载的壳聚糖纳米粒子原位凝胶系统是左氧氟沙星眼部传递的有效载体。