苯溴马隆与聚氧乙烯蓖麻油/乙醇/油酸/水微乳载体的相互作用研究

Effect of benzbromarone on the Cremophor EL/alcohol/oleic acid/water microemulsion carrier

为了探讨药物对纳米微乳载体的作用,制备了负载苯溴马隆的聚氧乙烯蓖麻油/乙醇/油酸/水微乳制剂。考察了该微乳体系在不同温度和离心条件下的稳定性及药物在微乳各组分中的溶解度及分布。并采用动态光散射、流变法、热分析以及红外光谱研究了不同药物浓度下微乳的微结构。结果表明:该载药微乳具有良好的物理稳定性。溶解度实验表明苯溴马隆主要分布在微乳水油两相的界面表面活性剂层。基于以上测试,显示苯溴马隆与微乳界面的两亲分子存在相互作用。从而使微乳的粒径略微减小,电导率增大,黏度变小,并破坏微乳相界面上的结合水,与聚氧乙烯蓖麻油的醚键有作用。而药物对微乳结构的影响将为苯溴马隆的微乳经皮制剂开发提供理论依据。

To investigate the effect of drug on microemulsion carrier,a microemulsion system with benzbromarone loaded has been developed using oleic acid,Cremophor EL,and alcohol as oil,surfactant,and co-surfactant,respectively.The stability test of microemulsions was performed at different temperatures and centrifugal forces,and the solubility and distribution of benzbromarone in microemulsion components were also measured.Moreover,microstructures of the microemulsions at different drug concentrations were characterized by a combination of techniques including rheological measurement,differential scanning calorimetry（DSC）,Fourier transform infrared spectroscopy（FT-IR）and dynamic light scattering（DLS）.The results showed that,microemulsions loaded with drug were proved to have physical stability,and solubility study demonstrated that benzbromarone was mainly located in the interfacial surfactant film between water and oil phase.Based on above characterizations,it could be deduced that it did have interactions between benzbromarone and amphiphilic molecules in the microemulsion interface,leading to a decrease in the size and viscosity of droplets,but an increase in conductivity.In addition,the incorporation of benzbromarone into microemulsion broke up bound water in phase interface and had effect on the ether bond of Cremophor EL.In order to obtain more theoretical foundation on the application of microemulsion system in transdermal delivery of benzbromarone,it proves useful to study the effect of drug on microemulsion microstructures with a series of above measures in detail.