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氟苯尼考固体脂质纳米粒混悬液的制备、表征及抗菌活性

Preparation, characterisation and antibacterial activity of a florfenicol-loaded solid lipid nanoparticle suspension.

作者信息

Wang Ting, Chen Xiaojin, Lu Mengmeng, Li Xihe, Zhou WenZhong

机构信息

Department of Preventive Veterinary Medicine, College of Veterinary Medicine, China Agricultural University, 2 Yuanmingyuan Road West, Beijing 100193, People's Republic of China.

Inner Mongolia Saikexing Reproductive Biotechnology Co. Ltd., Inner Mongolia University College of Life Sciences, Shengle Economic District, Helin Geer, Huhhot, Inner Mongolia 011517, People's Republic of China.

出版信息

IET Nanobiotechnol. 2015 Dec;9(6):355-61. doi: 10.1049/iet-nbt.2015.0012.

Abstract

A florfenicol-loaded solid lipid nanoparticle (FFC-SLN) suspension was prepared by hot homogenisation and ultrasonic technique. The suspension was characterised for its release profile, stability, toxicity, and the physicochemical properties of the nanoparticles. Antibacterial activity of the suspension was evaluated in vitro and in vivo. The results showed that the mean diameter, polydispersity index and zeta potential of the nanoparticles were 253 ± 3 nm, 0.409 ± 0.022 and 47.5 ± 0.21 mV, respectively. In vitro release profile showed the FFC-SLN suspension had sustained release effect. The minimum inhibition concentration values of the FFC-SLN suspension were 6 and 3 µg/mL against Staphylococcus aureus and Escherichia coli respectively, compared with 3.5 and 2 µg/mL of native florfenicol. The suspension was relatively stable at 4°C and less stable at room temperature during 9 months storage. Although the nanoparticle carriers exhibited cytotoxicity in cell cultures, the LD50 of the lyophilised dry power of the suspension was higher than 5 g/kg body weight. Mortality protection against E. coli lethal infection in mice showed that the nanoparticle suspension had much better efficacy (6/10) than native drug (1/10). These results indicate that FFC-SLN suspension could be a promising formulation in veterinary medicine.

摘要

通过热均质化和超声技术制备了载有氟苯尼考的固体脂质纳米粒(FFC-SLN)混悬液。对该混悬液的释放曲线、稳定性、毒性以及纳米粒的物理化学性质进行了表征。体外和体内评估了该混悬液的抗菌活性。结果表明,纳米粒的平均直径、多分散指数和zeta电位分别为253±3 nm、0.409±0.022和47.5±0.21 mV。体外释放曲线表明FFC-SLN混悬液具有缓释作用。FFC-SLN混悬液对金黄色葡萄球菌和大肠杆菌的最低抑菌浓度值分别为6和3 μg/mL,而天然氟苯尼考的最低抑菌浓度值分别为3.5和2 μg/mL。在9个月的储存期内,该混悬液在4°C时相对稳定,在室温下稳定性较差。虽然纳米粒载体在细胞培养中表现出细胞毒性,但该混悬液冻干干粉的半数致死量高于5 g/kg体重。小鼠对大肠杆菌致死感染的死亡率保护表明,纳米粒混悬液的疗效(6/10)比天然药物(1/10)好得多。这些结果表明,FFC-SLN混悬液可能是兽医学中一种有前景的制剂。

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