伊维菌素纳米乳透皮制剂的研究

doi:10.16431/j.cnki.1671-7236.2015.02.026

›› 2015, Vol. 42 ›› Issue (2): 401-407.doi: 10.16431/j.cnki.1671-7236.2015.02.026

伊维菌素纳米乳透皮制剂的研究

丁丹¹, 盛小莉², 梁孔贤¹, 许琦³, 刘卫^1,2,3

1. 华中科技大学生命科学与技术学院, 武汉 430074;
2. 华中科技大学国家纳米药物工程技术研究中心, 武汉 430074;
3. 武汉百思凯瑞纳米科技有限公司, 武汉 430074

收稿日期:2014-08-27 出版日期:2015-02-20 发布日期:2015-02-13
通讯作者: 刘卫 E-mail:wliu@hust.edu.cn
作者简介:丁丹(1990-),女,河南汝南人,硕士生,研究方向:纳米药物制剂,E-mail:dingdan900801@126.com
基金资助:
国家自然科学基金(31470968)

Study on Ivermectin Nanoemulsion for Transdermal Drug Delivery

DING Dan¹, SHENG Xiao-li², LIANG Kong-xian¹, XU Qi³, LIU Wei^1,2,3

1. College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan 430074, China;
2. National Engineering Research Center for Nanomedicine, Huazhong University of Science and Technology, Wuhan 430074, China;
3. Wuhan Best-carrier Nano Science and Technology Co., Ltd., Wuhan 430074, China

Received:2014-08-27 Online:2015-02-20 Published:2015-02-13

摘要/Abstract

摘要： 本试验研制伊维菌素纳米乳透皮制剂,并对其理化性能、稳定性、体外药物释放及透皮性能进行评价。采用三元相图筛选不同载药量的纳米乳,确定最佳载药量;采用响应面优化设计筛选纳米乳处方,考察了伊维菌素纳米乳的平均粒径、电位、形态、pH、黏度等性能;分别采用透析袋法和Franz扩散池法比较伊维菌素纳米乳透皮制剂与市售伊维菌素皮肤涂剂的体外释放行为和透皮性能。结果显示,载药量为2.00%时,纳米乳区域最大、最稳定;获得的优选处方为聚氧乙烯蓖麻油 :二乙二醇单乙基醚 :油酸乙酯 :伊维菌素 :水=26 :12 :7: 2: 53;所得伊维菌素纳米乳的平均粒径为18 nm;伊维菌素纳米乳在室温条件和4 ℃冰箱中保存1年仍稳定;其24 h皮肤累积渗透量和滞留量分别是市售伊维菌素皮肤涂剂的3.24和2.05倍。研究结果表明,研制的新型伊维菌素纳米乳透皮制剂具有制备工艺简便、稳定性好、透皮性能好等优点,具有很好的应用前景。

关键词: 伊维菌素; 纳米乳; 三元相图; 响应面优化设计; 体外药物释放; 透皮性能

Abstract: The aim of the study was to prepare ivermectin nanoemulsion for transdermal drug delivery.The physicochemical property,stability,in vitro drug release and transdermal property were evaluated.The optimal drug loading with good stability and larger nanoemulsion region was investigated by ternary phase diagram.The response surface methodology was used for selecting the optimal prescription.The average diameter,zeta potential,morphology,pH and viscosity were also investigated.In vitro drug release and transdermal property of ivermectin nanoemulsion and market ivermectin skin varnish were compared by dialysis bags and Franz diffusion cells.The nanoemulsion region was largest and most stable when the drug loading was 2.00%.The optimal prescription was Cremophor EL-35 :Transcutol HP :ethyl oleate :ivermectin :H₂O=26: 12: 7: 2: 53 and its average diameter was 18 nm.The ivermection nanoemulsion was stable when it was stored in 4 ℃ refrigerator and room temperature for 1 year.The cumulative permeation and retention of ivermectin nanoemulsion in 24 h were 3.24 and 2.05 times over the commercially available varnish,respectively.These results indicated that the ivermectin nanoemulsion had the advantages of simple preparation process,excellent stability and transdermal property,and had good application prospects.

Key words: ivermectin; nanoemulsion; ternary phase diagram; response surface methodology; in vitro drug release; transdermal property

中图分类号:

S859.7

丁丹, 盛小莉, 梁孔贤, 许琦, 刘卫. 伊维菌素纳米乳透皮制剂的研究[J]. , 2015, 42(2): 401-407.

DING Dan, SHENG Xiao-li, LIANG Kong-xian, XU Qi, LIU Wei. Study on Ivermectin Nanoemulsion for Transdermal Drug Delivery[J]. , 2015, 42(2): 401-407.

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伊维菌素纳米乳透皮制剂的研究

Study on Ivermectin Nanoemulsion for Transdermal Drug Delivery

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