非泼罗尼纳米乳的制备及理化性质与安全性分析

doi:10.11843/j.issn.0366-6964.2013.07.020

畜牧兽医学报 ›› 2013, Vol. 44 ›› Issue (7): 1140-1146.doi: 10.11843/j.issn.0366-6964.2013.07.020

非泼罗尼纳米乳的制备及理化性质与安全性分析

郭建军，欧阳五庆^*，李会芳，苏金辉，马志倩，李旭召，张莹

(西北农林科技大学动物医学院，杨凌 712100)

收稿日期:2013-01-30 出版日期:2013-07-23 发布日期:2013-07-23
通讯作者: 欧阳五庆，教授，博士生导师，主要从事新兽药研发、纳米生物技术和细胞生物学研究，E-mail：oywq506@sina.com
作者简介:郭建军(1984-)，男，河南焦作人，硕士生，主要从事新兽药开发研究，E-mail：gjjun81@126.com
基金资助:
陕西省重大科技创新专项基金项目(K332020916)

Preparation and Physical and Chemical Properties and Security Analysis of Fipronil Nanoemulsion

GUO Jian-jun, OUYANG Wu-qing^*, LI Hui-fang, SU Jin-hui, MA Zhi-qian, LI Xu-zhao, ZHANG Ying

(College of Veterinary Medicine, Northwest A&F University, Yangling 712100, China)

Received:2013-01-30 Online:2013-07-23 Published:2013-07-23

摘要/Abstract

摘要：

作者拟制备非泼罗尼纳米乳，并对其理化性质及安全性进行分析。以纳米乳的载药量、稳定性和毒性为考察指标，筛选合适的油相、表面活性剂，再利用伪三元相图选出最佳配方，制备出非泼罗尼纳米乳。用透射电镜观察非泼罗尼纳米乳的形态；用激光粒度分析仪测定其粒径分布范围、多分散系数(PDI)和Zeta电位；通过留样观察和加速试验考察其稳定性；通过皮肤毒性试验和急性毒性试验评估其安全性；通过改良的Franz扩散装置考察其透皮性。结果显示非泼罗尼纳米乳最佳配方：非泼罗尼1.2%，肉桂醛8.0%，聚氧乙烯醚蓖麻油 32.0%，蒸馏水58.8%。其呈规则的圆球形，粒径分布在5～24 nm，平均粒径11.5 nm，PDI为0.218，Zeta电位为－20.6 mV，稳定性良好。皮肤毒性试验、急性毒性试验和透皮试验表明，该纳米乳有良好的安全性和透皮效果。成功研制了非泼罗尼纳米乳，其稳定性好，安全性高，透皮性好。

Abstract:

The purpose of this study was to establish Fipronil nanoemulsion formula and to analyse its quality and security. The appropriate oil phase and surfactant were selected according to the drug loading, stability and toxicity of nanoemulsion and the optimum formula was designed using pseudo-ternary phase diagram. The configuration was measured by TEM and the particle size, polydispersity and zeta potential were measured by LPSA. The stability was tested by high speed centrifugation and optic observation. Its security was evaluated in this study by dermal acute toxicity and LD₅₀. Evaluation of its transdermal permeability was measured by utilizing modified Franz diffusion device. The optimum formula of Fipronil nanoemulsion was composed of 1.2% (w/w) Fipronil, 8.0% (w/w) cinnamaldehyde, 32.0% (w/w) EL-40 and 58.8% (w/w) distilled water. The shape of Fipronil nanoemulsion droplet was spherical under TEM and the particle size ranged from 5 to 24 nm, with the average diameter of 11.5 nm. The PDI was 0.218 and the Zata potential was －20.6 mV. It was stable. The security test demonstrated that its dermal acute toxicity test was good and LD₅₀ was 2 626 mg·kg^-1, therefore it was Low-toxic. Its percutaneous penetration was enhanced. The Fipronil nanoemulsion was successfully prepared, it was stable and Low-toxic. Its percutaneous penetration was well.

中图分类号:

S859.53

郭建军，欧阳五庆，李会芳，苏金辉，马志倩，李旭召，张莹. 非泼罗尼纳米乳的制备及理化性质与安全性分析[J]. 畜牧兽医学报, 2013, 44(7): 1140-1146.

GUO Jian-jun, OUYANG Wu-qing, LI Hui-fang, SU Jin-hui, MA Zhi-qian, LI Xu-zhao, ZHANG Ying. Preparation and Physical and Chemical Properties and Security Analysis of Fipronil Nanoemulsion[J]. ACTA VETERINARIA ET ZOOTECHNICA SINICA, 2013, 44(7): 1140-1146.

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非泼罗尼纳米乳的制备及理化性质与安全性分析

Preparation and Physical and Chemical Properties and Security Analysis of Fipronil Nanoemulsion

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