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Salutary influence of gemifloxacin mesylate nanocubosomes based-in situ ocular gel as a novel approach for the management of experimental keratitis induced by MRSA
Journal of Drug Delivery Science and Technology ( IF 4.5 ) Pub Date : 2023-10-08 , DOI: 10.1016/j.jddst.2023.105012
Ghada Ahmed El-Emam , Amira Motawea , Walaa Ebrahim Abd El Hady , Sameh Saber , Ahmed A.E. Mourad , Heba A. Ramadan , Ahmed M. El-Baz

In the era of Methicillin-resistant Staphylococcus aureus (MRSA) resulting in the ineffectiveness of antibiotics is of keen interest to researchers in up-to-date scenarios. The current study aims to formulate water-soluble drug (Gemifloxacin) loaded nanocubosomes via melt dispersion emulsification method using glyceryl mono oleate/poloxamer 407 in different ratios. Firstly, the optimized formula (F6) was evaluated for surface morphology, particle size, polydispersity index, zeta potential, drug entrapment efficiency%, compatibility studies, and in vitro release. Secondly, the optimized formulation of nanocubosomes was laden as in situ gel and evaluated for gelling effect, in vitro release, drug content, stability study, and antimicrobial activity. The optimized nanocubosomes F6 showed a particle size of less than 200 nm, a zeta potential −26.6 ± 1.3 mV, and a high entrapment efficiency of 96.62 ± 2.35%. The developed in situ gel (F6) shows prolonged drug release and good stability. Our objectives in that study are to investigate the effectiveness of that novel approach for the management of corneal lesions and inflammation in a rat model of MRSA keratitis as well as in vitro estimation for their MIC. Results showed greater potency by having lower MICs than Gemifloxacin solution and significant reductions in corneal opacity and inflammation score in rats treated with GEM-loaded nanocubosomes compared to those treated with Gemifloxacin solution. Histopathological analysis demonstrated a preservation of the normal corneal structure in the GEM-loaded nanocubosomes group. It is clear from the above-performed studies that the prepared in situ gel would afford a profitable treatment for keratitis with a lack of irritancy.



中文翻译:

基于原位眼用凝胶的甲磺酸吉米沙星纳米立方体作为治疗由 MRSA 引起的实验性角膜炎的新方法的有益影响

在耐甲氧西林金黄色葡萄球菌(MRSA) 导致抗生素无效的时代,最新情况引起了研究人员的浓厚兴趣。本研究旨在使用不同比例的单油酸甘油酯/泊洛沙姆 407,通过熔融分散乳化法配制负载水溶性药物(吉米沙星)的纳米立方体。首先,对优化配方(F6)的表面形貌、粒径、多分散指数、zeta电位、药物包封率%、相容性研究和体外释放进行评估。其次,将优化的纳米立方体制剂装载为原位凝胶,并评估其凝胶效果、体外释放、药物含量、稳定性研究和抗菌活性。优化后的纳米立方体F6的粒径小于200  nm ,zeta电位为-26.6 ± 1.3 mV,包封效率高达96.62 ± 2.35%。开发的原位凝胶(F6)显示出较长的药物释放和良好的稳定性。我们在该研究中的目的是调查这种新方法在 MRSA 角膜炎大鼠模型中治疗角膜病变和炎症的有效性,以及体外估计其MIC 结果显示,与用吉米沙星溶液治疗的大鼠相比,用 GEM 负载的纳米立方体治疗的大鼠具有比吉米沙星溶液更低的 MIC,并且角膜混浊和炎症评分显着降低。组织病理学分析表明,负载 GEM 的纳米立方体组保留了正常角膜结构。从上述研究可以清楚地看出,制备的原位凝胶将为角膜炎提供有效的治疗,且无刺激性。

更新日期:2023-10-08
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