环吡酮胺纳米乳的体外抑菌活性及透皮性能研究  

Study on Antifungal Activity of Ciclopirox Olamine Nanoemulsion and Its Transdermal Permeability in vitro

作　　者：宋冠男[1] 欧阳五庆[1] 郭建军[1] 郑星星[1] 周莹[1] 

机构地区：[1]西北农林科技大学动物医学院,杨凌712100

出　　处：《畜牧兽医学报》2013年第3期453-458,共6页ACTA VETERINARIA ET ZOOTECHNICA SINICA

基　　金：陕西省重大科技创新专项基金项目(K332020916)

摘　　要：本研究旨在考察环吡酮胺纳米乳的体外药效及经皮渗透性能,为其临床应用提供试验依据。用微量稀释法对环吡酮胺纳米乳的体外抑菌活性进行考察;利用改良的Franz扩散装置对环吡酮胺纳米乳的体外经皮渗透能力进行评价。体外抑菌活性试验结果表明,环吡酮胺纳米乳对白色念珠菌、酵母菌和金黄色葡萄球菌的MIC分别是0.125、0.250、16.000μg.mL-1,优于环吡酮胺溶液和联苯苄唑溶液,说明以纳米乳作为药物载体,提高了环吡酮胺的抑菌活性。体外经皮渗透性试验结果表明,环吡酮胺纳米乳原液、含2%、5%氮酮的环吡酮胺纳米乳液的经皮渗透速率分别为(22.381±0.114)、(134.573±0.012)、(50.350±0.001)μg.cm-2.h-1,而环吡酮胺20%乙醇溶液的渗透速率为(10.891±0.062)μg.cm-2.h-1,说明环吡酮胺纳米乳提高了药物的经皮渗透性(P<0.01),而促渗剂氮酮的加入,能够进一步提高药物的经皮渗透能力(P<0.01)。纳米乳作为环吡酮胺药物的载体,提高了其抑菌活性及经皮渗透能力,为环吡酮胺纳米乳剂型的临床应用提供了理论依据。A series of tests were conducted to investigate the drug efficacy and transdermal speed of ciclopirox olamine nanoemulsion in vitro and provide experimental basis for clinical application. Antifungal activity test of ciclopirox olamine in vitro was conducted by using the microdilution method and evaluation of its transdermal permeability was by utilizing modified Franz diffusion device. The results of antifungal activity test in vitro showed that the MIC to Candida albicans, Saccharomyces cerevisiae and Staphylococcus aureus was 0. 125, 0. 250 and 16. 000μg · mL^-1 , respectively, which was better than results of ciclopirox olamine solution and bifonazole solution obviously. It is manifest that nanoemulsion as a kind of drug carrier can improve the antifungal activity of ciclopirox olamine. The results of transdermal permeability of ciclopirox olamine nanoemulsion in vitro test illuminate that the transdermal rate of ciclopirox olamine nanoemulsion and ones with 2%, 5% azone was （22. 381 ± 0. 114）, （134. 573＋0. 012）, （50. 350±0. 001） /μg · mL^-2 · h^-1 , respectively, whereas the transderreal rate of eiclopirox with 20± ethanol solution was （10. 891±0. 062） μg · mL^-2 · h^-1. It shows that ciclopirox olamine nanoemulsion enhances its percutaneous penetration （P〈0.01） and it can further improve its transdermal ability in vitro when the azone was added （P〈0.01）. Overall, nanoemulsion as the carrier of ciclopirox olamine can improve its antifungal activity and transder mal speed, which provides a theoretical basis for clinical application of ciclopirox olamine nanoemulsion.

关 键 词：纳米乳 环吡酮胺 抑菌活性 经皮渗透 药物剂型 

分 类 号：R944.9[医药卫生—药剂学]