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首页> 外文期刊>International Journal of Pharmaceutics >Investigation of surfactant/cosurfactant synergism impact on ibuprofen solubilization capacity and drug release characteristics of nonionic microemulsions
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Investigation of surfactant/cosurfactant synergism impact on ibuprofen solubilization capacity and drug release characteristics of nonionic microemulsions

机译：表面活性剂/助表面活性剂协同作用对布洛芬非离子微乳液增溶能力和药物释放特性影响的研究

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The current study investigates the performances of the multicomponent mixtures of nonionic surfactants regarding the microemulsion stabilisation, drug solubilization and in vitro drug release kinetic. The primary surfactant was PEG-8 caprylic/capric glycerides (Labrasol?). The cosurfactants were commercially available mixtures of octoxynol-12 and polysorbate 20 without or with the addition of PEG-40 hydrogenated castor oil (Solubilisant gamma? 2421 and Solubilisant gamma? 2429, respectively). The oil phase of microemulsions was isopropyl myristate. Phase behaviour study of the pseudo-ternary systems Labrasol?/cosurfactant/oil/water at surfactant-to-cosurfactant weight ratios (K m) 40:60, 50:50 and 60:40, revealed a strong synergism in the investigated tensides mixtures for stabilisation of microemulsions containing up to 80% (w/w) of water phase at surfactant +cosurfactant-to-oil weight ratio (SCoS/O) 90:10. Solubilization of a model drug ibuprofen in concentration common for topical application (5%, w/w) was achieved at the water contents below 50% (w/w). Drug free and ibuprofen-loaded microemulsions M1-M6, containing 45% (w/w) of water phase, were prepared and characterized by polarized light microscopy, conductivity, pH, rheological and droplet size measurements. In vitro ibuprofen release kinetics from the microemulsions was investigated using paddle-over-enhancer cell method and compared with the commercial 5% (w/w) ibuprofen hydrogel product (Deep Relief?, Mentholatum Company Ltd., USA). The investigated microemulsions were isotropic, low viscous Bingham-type liquids with the pH value (4.70-6.61) suitable for topical application. The different efficiency of the tensides mixtures for microemulsion stabilisation was observed, depending on the cosurfactant type and K m value. Solubilisant gamma? 2429 as well as higher K m (i.e., lower relative content of the cosurfactant) provided higher surfactant/cosurfactant synergism. The drug molecules were predominantly solubilized within the interface film. The amount of drug released from the formulations M3 (10.75%, w/w) and M6 (13.45%, w/w) (K m 60:40) was limited in comparison with the reference (22.22%, w/w) and follows the Higuchi model. Microemulsions M2 and M5 (K m 50:50) gave zero order drug release pattern and ～15% (w/w) ibuprofen released. The release profiles from microemulsions M1 and M4 (K m 40:60) did not fit well with the models used for analysis, although the amounts of ibuprofen released (24.47%, w/w) and 17.99% (w/w), respectively) were comparable to that of the reference hydrogel. The drug release mechanism was related with the surfactant/cosurfactant synergism, thus the lower efficiency of the tensides corresponded to the faster drug release.
机译：当前的研究调查了非离子表面活性剂多组分混合物在微乳液稳定，药物增溶和体外药物释放动力学方面的性能。主要的表面活性剂是PEG-8辛酸/癸酸甘油酯（Labrasol？）。助表面活性剂是可商购获得的辛氧基醇12和聚山梨酯20的混合物，不加或不加PEG-40氢化蓖麻油（分别为增溶剂γ2421和增溶剂γ2429）。微乳液的油相是肉豆蔻酸异丙酯。在表面活性剂与助表面活性剂重量比（K m）为40：60、50：50和60:40的拟三元体系Labrasol®/助表面活性剂/油/水的相行为研究表明，所研究的表面活性剂混合物具有很强的协同作用用于稳定表面活性剂与助表面活性剂与油的重量比（SCoS / O）为90:10的水含量高达80％（w / w）的微乳液。当水含量低于50％（w / w）时，可达到局部应用常用浓度的模型药物布洛芬（5％，w / w）的增溶作用。制备了无药且布洛芬载有45％（w / w）水相的微乳M1-M6，并通过偏光显微镜，电导率，pH，流变学和液滴尺寸测量对其进行了表征。使用增强桨法研究了微乳液的体外布洛芬释放动力学，并将其与市售的5％（w / w）布洛芬水凝胶产品（Deep Relief？，Mentholatum Company Ltd.，美国）进行了比较。研究的微乳状液是各向同性的低粘度宾厄姆型液体，pH值（4.70-6.61）适合局部应用。观察到表面活性剂混合物对微乳液稳定的不同效率，这取决于助表面活性剂类型和K m值。增溶剂γ？ 2429以及较高的K m（即较低的辅助表面活性剂相对含量）提供了较高的表面活性剂/辅助表面活性剂协同作用。药物分子主要溶解在界面膜内。与参考文献（22.22％，w / w）相比，制剂M3（10.75％，w / w）和M6（13.45％，w / w）（K m 60:40）释放的药物量受到限制。遵循Higuchi模型。微乳M2和M5（K m 50:50）产生零级药物释放模式，布洛芬释放量约为15％（w / w）。尽管布洛芬的释放量分别为（24.47％，w / w）和17.99％（w / w），但微乳液M1和M4的释放曲线（K m 40:60）与用于分析的模型不太吻合。 ）与参考水凝胶相当。药物释放机理与表面活性剂/助表面活性剂的协同作用有关，因此表面活性剂的较低效率对应于较快的药物释放。

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