OBJECTIVE Impetigo is a common and highly contagious bacterial skin infection that mostly affects young children and infants. Herein, we report the development of a thermosensitive and bioadhesive in-situ hydrogel-forming system containing cephalexin-loaded nanoparticles (NPs) suitable for antibacterial drug delivery. METHODS The nanohydrogel was formulated using drug-loaded NPs and characterized by its physicochemical characteristics. Antibacterial activities of the cephalexin NPs and nanohydrogel were examined in vitro against Staphylococcus aureus (S. aureus). The ex vivo drug permeation study was performed using rat skin. Finally, this formulation was tested for in vivo antibacterial activity using superficial skin infections in rats. RESULTS The mean size and entrapment efficiency of the NPs were found to be 178 nm and 58%, respectively. The transmission electron microscopy analysis verified the formation of spherical NPs. The drug-loaded NPs showed an enhanced eradication effect against S. aureus according to the declined MIC values in comparison with the untreated drug. The ex vivo permeation profile of the cephalexin nanohydrogel showed a slow release pattern for 8 h. When applied on rat skin for 6 days, the nanohydrogel exhibited a superior antibacterial activity with normal hair growth and skin appearance as compared to the plain drug hydrogel. CONCLUSIONS These findings suggested that the nanohydrogel could serve as a valuable drug delivery platform against superficial bacterial infections.

中文翻译：

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新型热敏性和生物粘附性头孢氨苄纳米水凝胶的制备和表征：局部抗菌释放的有前途的平台。

目的脓疱病是一种常见的且具有高度传染性的细菌性皮肤感染，主要影响幼儿和婴儿。在此，我们报告了一种热敏性和生物粘附性原位水凝胶形成系统的开发，该系统包含适用于抗菌药物递送的头孢氨苄负载的纳米颗粒（NP）。方法采用载药纳米粒制备纳米水凝胶，并对其理化特性进行表征。在体外检查了头孢氨苄NPs和纳米水凝胶对金黄色葡萄球菌（金黄色葡萄球菌）的抗菌活性。使用大鼠皮肤进行离体药物渗透研究。最后，使用大鼠的浅表皮肤感染测试了该制剂的体内抗菌活性。结果发现NP的平均大小和包封效率分别为178 nm和58％。透射电子显微镜分析证实了球形NP的形成。与未处理的药物相比，根据降低的MIC值，载有药物的NP对金黄色葡萄球菌具有增强的根除效果。头孢氨苄纳米水凝胶的离体渗透曲线显示了8 h的缓慢释放模式。与普通药物水凝胶相比，当在大鼠皮肤上使用6天时，纳米水凝胶表现出优异的抗菌活性，具有正常的毛发生长和皮肤外观。结论这些发现表明纳米水凝胶可以作为抵抗浅表细菌感染的有价值的药物递送平台。与未处理药物相比，金黄色葡萄球菌的MIC值下降。头孢氨苄纳米水凝胶的离体渗透曲线显示了8 h的缓慢释放模式。与普通药物水凝胶相比，当在大鼠皮肤上使用6天时，纳米水凝胶表现出优异的抗菌活性，具有正常的毛发生长和皮肤外观。结论这些发现表明纳米水凝胶可以作为抵抗浅表细菌感染的有价值的药物递送平台。与未处理药物相比，金黄色葡萄球菌的MIC值下降。头孢氨苄纳米水凝胶的离体渗透曲线显示了8 h的缓慢释放模式。与普通药物水凝胶相比，当在大鼠皮肤上使用6天时，纳米水凝胶表现出优异的抗菌活性，具有正常的毛发生长和皮肤外观。结论这些发现表明纳米水凝胶可以作为抵抗浅表细菌感染的有价值的药物递送平台。