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壳聚糖-牛血清白蛋白-卡波姆 940 纳米凝胶用于莫匹罗星经皮给药:通过放射性标记评估体外渗透和细胞结合能力。

Chitosan-bovine serum albumin-Carbopol 940 nanogels for mupirocin dermal delivery: ex-vivo permeation and evaluation of cellular binding capacity via radiolabeling.

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Izmir Katip Celebi University, Izmir, Turkey.

Department of Pharmaceutical Technology, Faculty of Pharmacy, Ege University, Izmir, Turkey.

出版信息

Pharm Dev Technol. 2021 Oct;26(8):852-866. doi: 10.1080/10837450.2021.1948570. Epub 2021 Jul 11.

Abstract

The goal of this study was to develop and examine the nanogel-based topical delivery system of mupirocin. Nanogels were prepared with chitosan and bovine serum albumin by ionic gelation and Carbopol 940 was added to improve the gelling/adhesive properties. Detailed characterization studies were performed and the cellular binding capacity of radiolabeled nanogels was investigated on CCD-1070Sk cell lines. Results indicate the successful formation of nanogels with particle size and zeta potential ranged between 341.920-603.320 nm and 13.120-24.300 mV, respectively. The mechanical and rheological studies proved pseudoplastic and strong elastic gel behavior (G' > G''). Mupirocin was successfully entrapped into nanogels with a ratio of more than 95% and the loaded drug was slowly released up to 93.89 ± 3.07% within 24 h. The penetration and permeation percentages of mupirocin were very low (1.172 ± 0.202% and 0.161 ± 0.136%) indicating the suitability of nanogels for dermal use against superficial skin infections. The microbiological studies pointed out the effectiveness of nanogels against strains. Nanogels did not show toxicity signs and the cell binding capacity of radiolabeled formulations was found to be higher than [Tc]NaTcO to CCD-1070Sk cell line. Overall, mupirocin nanogels might be considered as a potential and safe topical treatment option for bacterial skin infections.

摘要

本研究的目的是开发和研究莫匹罗星的纳米凝胶局部递药系统。纳米凝胶是通过离子凝胶化法用壳聚糖和牛血清白蛋白制备的,并添加 Carbopol 940 以改善凝胶/粘性特性。进行了详细的特征研究,并研究了放射性标记的纳米凝胶在 CCD-1070Sk 细胞系上的细胞结合能力。结果表明成功地形成了粒径和 Zeta 电位分别在 341.920-603.320nm 和 13.120-24.300mV 之间的纳米凝胶。机械和流变学研究证明了假塑性和强弹性凝胶行为(G' > G '')。莫匹罗星成功地包封在纳米凝胶中,包封率超过 95%,负载药物在 24 小时内缓慢释放,达到 93.89 ± 3.07%。莫匹罗星的渗透和透皮百分比非常低(1.172 ± 0.202%和 0.161 ± 0.136%),表明纳米凝胶适用于治疗浅层皮肤感染的皮肤用药。微生物学研究表明纳米凝胶对 株有效。纳米凝胶未显示出毒性迹象,放射性标记制剂的细胞结合能力高于 [Tc]NaTcO 对 CCD-1070Sk 细胞系。总体而言,莫匹罗星纳米凝胶可被视为治疗细菌皮肤感染的潜在安全的局部治疗选择。

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