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浙江大学学报（农业与生命科学版）
浙江大学学报(农业与生命科学版)  2012, Vol. 38 Issue (6): 693-699    DOI: 10.3785/j.issn.1008-9209.2012.01.051
生物科学与技术     
  恩诺沙星纳米乳的制备及其质量评价
  杨雪峰[1]， 齐永华， 宁红梅， 王清华  
河南科技学院 动物科学学院，河南 新乡 453003
Preparation and quality evaluation of enrofloxacin nanoemulsion
YANG Xue-feng*, QI Yong-hua, NING Hong-mei, WANG Qing-hua
College of Animal Science, Henan Institute of Science and Technology, Xinxiang, Henan 453003, China
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摘要： 为制备恩诺沙星纳米乳，首先通过滴定法绘制伪三元相图，研究不同表面活性剂、助表面活性剂、表面活性剂和助表面活性剂质量比 (Km) 形成纳米乳的区域，筛选出最佳制备处方，并对制备的恩诺沙星纳米乳进行质量评价. 结果表明：最佳的纳米乳处方为肉豆蔻酸异丙酯 (IPM)、聚氧乙烯蓖麻油-40 (EL-40)、乙酸 (HAc) 和水，其中Km为3∶2，各成分的质量分数为恩诺沙星15 %，IPM 3 %，EL-40和HAc 48 %，蒸馏水34 %；所制备的恩诺沙星纳米乳为O/W型，澄明均一，平均粒径为 (22.45 ± 2.92) nm，粒径呈正态分布，pH 4.36；该纳米乳对大肠杆菌ATCC25922和金黄色葡萄球菌ATCC25923的最小抑菌浓度 (MIC) 均为其原料药MIC的1/2；在离心试验和温度试验条件下，未见乳液分层、破乳和药物析出现象. 结果显示，恩诺沙星纳米乳制备工艺简单、溶解度高、抗菌活性强、稳定性好.
Abstract:   Enrofloxacin is the first fluoroquinolone antimicrobial agent solely for veterinary use. The drug has a broad spectrum of activity, being active against both Gram-positive, Gram-negative bacteria and mycoplasmas. Now the traditional clinical dosage forms include powder, injection, solution and suspension, and so on. Some new dosage forms such as nanoparticles, microsphere, liposomes, β-cyclodextrin inclusion complex, sustained-release granules, microencapsulation and microcapsules have been also studied and reported accompanying with the development of the new preparation technique, but the research about enrofloxacin nanoemulsion has not yet been reported. The low water solubility is still an important limiting factor hampering enrofloxacin administration and the development of the novel preparation. So, we aimed to prepare enrofloxacin nanoemulsion with enrofloxacin as a model drug and nanoemulsion as a drug carrier by incorporating enrofloxacin into a nanoemulsion to improve its water solubility. In order to screen an optimal prescription for preparing enrofloxacin nanoemulsion, the oil phase was screened among isopropyl myristate (IPM), acetic ether, soybean oil and peanut oil; the surfactant was screened among polyoxyl 40 hydrogenated castor oil, polyoxyethylene castor oil (EL-40), Tween-80, lecithin and Span 80; the cosurfactant was screened among ethanol, 1, 2-propanediol, glycerin, acetic acid (HAc), lactic acid and propanoic acid; and the mass ratio (Km) of surfactant to cosurfactant was screened among 3∶1, 3∶2 and 3∶3, respectively. A pseudo-ternary phase diagram was established to investigate the effect of various compositions on the formation region of the nanoemulsion. The phase diagram was obtained by an aqueous titration method with one axis representing the mixture of surfactant and cosurfactant named as combined surfactant (Smix), another representing the oil phase, and the third representing the water phase. Based on the nanoemulsion region, the optimal prescription was screened. Then, enrofloxacin nanoemulsion was prepared according to the screened prescription and its quality was evaluated. The results showed that the optimized formulation was IPM as oil phase (Table 1), EL-40 as surfactant (Fig. 1B), HAc as cosurfactant (Fig. 2A), the distilled water as the aqueous phase. In this screened prescription, Km was 3∶2 (Fig. 3B), and it contained enrofloxacin of 15 %, IPM of 3 %, Smix of 48 %, and distilled water of 34 %. According to the prescription, the prepared enrofloxacin nanoemulsion was with a transparent and uniform appearance, the structural type of oil-in-water, and the spherical droplet observed by transmission electron microscope (Fig. 4). The mean size of the nanoemulsion droplet was (22.45 ± 2.92) nm with Gaussian distribution verified by laser scattering analyzer (Fig. 5), and the value of pH was 4.63, and the minimal inhibitory concentration (MIC) against Escherichia coli ATCC25922 and Staphylococcus aureus ATCC25923 was both 1/2 times the MIC of the crude drug (Table 2). The nanoemulsion was not found the phenomenon of the delamination, demulsification and medicine leakage under the centrifugalization trial and the thermal test.  The results above suggest that the optimal preparation procedure of enrofloxacin nanoemulsion is simple and practicable. Enrofloxacin nanoemulsion has a high solubility, strong antibacterial activity, good stability and benefit administration of group drinking water, and effectually overcome the defects such as a poor water-solubility and instability to preserve the traditional dosage form of enrofloxacin. It can be used as a new type of nano-antimicrobial drug for veterinary clinic.
出版日期: 2012-11-20
基金资助:

河南科技学院博士科研启动经费资助项目(09006).
通讯作者: 杨雪峰，E-mail: yangxuefeng2003@126.com   
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引用本文:

杨雪峰,齐永华， 宁红梅， 王清华.   恩诺沙星纳米乳的制备及其质量评价[J]. 浙江大学学报(农业与生命科学版), 2012, 38(6): 693-699.

YANG Xue-feng*, QI Yong-hua, NING Hong-mei, WANG Qing-hua. Preparation and quality evaluation of enrofloxacin nanoemulsion. , 2012, 38(6): 693-699.

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http://www.zjujournals.com/agr/CN/10.3785/j.issn.1008-9209.2012.01.051    或    http://www.zjujournals.com/agr/CN/Y2012/V38/I6/693

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