Department of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Erzincan Binali Yıldırım University, Erzincan, Turkey.
J Ocul Pharmacol Ther. 2022 Jul-Aug;38(6):412-423. doi: 10.1089/jop.2022.0008. Epub 2022 Jun 8.
In the treatment of severe cases of bacterial keratitis, conventional eye drops containing antibiotics should be applied daily and very frequently. The aim of this study is to develop low-dose high-effect formulations with the prepared nanostructured lipid carrier (NLC) formulations to reduce antibiotic resistance and increase patient compliance. NLC formulations were loaded with besifloxacin HCl (BHL) and the besifloxacin HCl: sulfobutyl ether beta-cyclodextrin (SBE-CD) complex. Positive charge was gained with chitosan, and corneal permeation and resolubility were increased with SBE-CD. characterization studies, permeability studies, and cytotoxicity and transport studies were carried out. In this study, it was found that SBE-CD increased BHL's solubility by 8-fold based on phase solubility studies. The optimized NLCs were small in size (13.63-16.09 nm) with a low polydispersity index (0.107-0.181) and adequate BHL drug loading efficiency. release studies showed that formulations were released approximately for 8 h and at levels over the minimum inhibitory concentration of and . NLC formulations had a better corneal permeation rate than the marketed product during 6 h of studies. According to and data, it was determined that the most favorable NLC formulation was the formulation containing BHL/SBE-CD that was covered with chitosan. It has the highest drug loading capacity and one of the highest corneal passage levels, along with desired drug release. The formulation containing BHL/SBE-CD and chitosan can be a potential alternative for the treatment of bacterial keratitis.
在治疗严重细菌性角膜炎时,应每日并非常频繁地使用含有抗生素的常规眼药水。本研究旨在开发低剂量、高疗效的制剂,使用制备的纳米结构化脂质载体(NLC)制剂来降低抗生素耐药性并提高患者的依从性。NLC 制剂负载盐酸贝西沙星(BHL)和盐酸贝西沙星:磺丁基醚-β-环糊精(SBE-β-CD)复合物。用壳聚糖获得正电荷,并用 SBE-β-CD 提高角膜渗透性和溶解性。进行了表征研究、渗透性研究、细胞毒性和转运研究。在这项研究中,发现 SBE-β-CD 根据相溶解度研究将 BHL 的溶解度提高了 8 倍。优化的 NLC 粒径较小(13.63-16.09nm),多分散指数低(0.107-0.181),BHL 药物载药量效率高。释放研究表明,制剂约释放 8 小时,释放水平超过和的最低抑菌浓度。在 6 小时的研究中,NLC 制剂的角膜透过率优于市售产品。根据和数据,确定最有利的 NLC 制剂是用壳聚糖覆盖的包含 BHL/SBE-β-CD 的制剂。它具有最高的载药量和最高的之一角膜透过水平,同时具有理想的药物释放。包含 BHL/SBE-β-CD 和壳聚糖的制剂可能是治疗细菌性角膜炎的一种潜在替代方法。