Abstract：
To formulate and optimize Ozenoxacin nano-emulsion using Quality by Design (QbD) concept by means of Box-Behnken Design (BBD) and converting it to a gel to form Ozenoxacin nano-emulgel followed by physico-chemical, in-vitro, ex-vivo and in-vivo evaluation. This study demonstrates the application of QbD methodology for the development and optimization of an effective topical nanoemulgel formulation for the treatment of Impetigo focusing on the selection of appropriate excipients, optimization of formulation and process variables, and characterization of critical quality attributes. BBD was used to study the effect of \"% of oil, % of Smix and homogenization speed\" on critical quality attributes \"globule size and % entrapment efficiency\" for the optimisation of Ozenoxacin Nano-emulsion. Ozenoxacin loaded nano-emulgel was characterized for \"description, identification, pH, specific gravity, amplitude sweep, viscosity, assay, organic impurities, antimicrobial effectiveness testing, in-vitro release testing, ex-vivo permeation testing, skin retention and in-vivo anti-bacterial activity\". In-vitro release and ex-vivo permeation, skin retention and in-vivo anti-bacterial activity were found to be significantly (p < 0.01) higher for the nano-emulgel formulation compared to the innovator formulation (OZANEX™). Antimicrobial effectiveness testing was performed and found that even at 70% label claim of benzoic acid is effective to inhibit microbial growth in the drug product. The systematic application of QbD principles facilitated the successful development and optimization of a Ozenoxacin Nano-Emulsion. Optimised Ozenoxacin Nano-Emulgel can be considered as an effective alternative and found to be stable at least for 6 months at 40 °C / 75% RH and 30 °C / 75% RH.
摘要：
通过Box-BehnkenDesign（BBD）使用质量设计（QbD）概念配制和优化奥替诺沙星纳米乳液，并将其转化为凝胶以形成奥替诺沙星纳米乳液，然后进行物理化学，体外，离体和体内评估。这项研究证明了QbD方法在开发和优化治疗Impetigo的有效局部纳米乳凝胶制剂中的应用，重点是选择合适的赋形剂，配方和工艺变量的优化，和关键质量属性的表征。BBD用于研究油的影响，Smix和均质化速度“关于关键质量属性”的“小球大小和包封效率百分比”，用于优化奥扎诺沙星纳米乳液。负载奥替诺沙星的纳米乳液的特征为“描述”，identification,pH值,比重,振幅扫描,粘度,分析,有机杂质，抗菌效果测试，体外释放测试，离体渗透测试，皮肤滞留和体内抗菌活性。“体外释放和离体渗透，发现与创新制剂(OZANEX™)相比,纳米乳液制剂的皮肤保留和体内抗菌活性显著(p<0.01)更高。进行抗微生物效果测试,发现即使在70%的标签上,苯甲酸的声明也有效地抑制药物产品中的微生物生长。QbD原理的系统应用促进了奥替诺沙星纳米乳液的成功开发和优化。优化的奥替诺沙星纳米乳液凝胶可以被认为是有效的替代品，并且发现在40°C/75％RH和30°C/75％RH下至少稳定6个月。
