载有槲皮素的微乳液的配方、特性描述及经体外/体内评估的用于局部应用。
Formulation, characterization, and in vitro/ex vivo evaluation of quercetin-loaded microemulsion for topical application.
机构信息
a Department of Chemistry, Faculty of Science , Arak University , Arak , Iran.
b Department of Pharmaceutics, School of Pharmacy , Nanotechnology Research Center, Jundishapur University of Medical Sciences , Ahvaz , Iran.
出版信息
Pharm Dev Technol. 2018 Oct;23(8):741-750. doi: 10.1080/10837450.2016.1263995. Epub 2016 Dec 9.
The aim of this study was to develop a new microemulsion formulation for topical application of poorly soluble drug named quercetin. In order to design suitable microemulsion system, the pseudo-ternary phase diagrams of microemulsion systems were constructed at different surfactant/co-surfactant ratios using tween 80 as surfactant, transcutol P as a co-surfactant and oleic acid as an oil phase. Some physicochemical properties such as droplet size, density, refractive index, electrical conductivity, pH, surface tension, and viscosity of the microemulsion systems were measured at 298.15 K. The average hydrodynamic droplet size of the optimized microemulsions was obtained by dynamic light scattering method. Morphology assessment of the optimized quercetin-loaded microemulsion by transmission electron microscopy analysis indicated that the particles have the size of about 25 nm and spherical with narrow size distribution. Equilibrium solubility, in vitro drug release at a 24 h time period, release kinetic evaluation as well as ex vivo permeation and retention of quercetin-loaded microemulsions through rat skin has been investigated. The obtained results showed a slow release behavior without any transdermal delivery. Most of the formulations fitted best with zero-order kinetic model with a non-Fickian mechanisms. This study illustrated that the proposed QU-microemulsion has a good potential for use in sunscreen formulations. [Formula: see text].
本研究旨在开发一种新的微乳制剂,用于局部应用名为槲皮素的难溶性药物。为了设计合适的微乳体系,使用吐温 80 作为表面活性剂、丙二醇作为助表面活性剂和油酸作为油相,在不同的表面活性剂/助表面活性剂比例下构建了微乳体系的伪三元相图。在 298.15 K 下测量了微乳体系的一些物理化学性质,如粒径、密度、折射率、电导率、pH 值、表面张力和粘度。通过动态光散射法获得了优化微乳的平均水动力粒径。通过透射电子显微镜分析对载药微乳进行形态评价,结果表明颗粒尺寸约为 25nm,呈球形,分布较窄。考察了载药微乳的平衡溶解度、24 小时内的体外药物释放、释放动力学评价以及通过大鼠皮肤的体外渗透和保留。结果表明,微乳具有缓慢释放行为,没有任何经皮递送。大多数制剂与零级动力学模型拟合最好,具有非菲克扩散机制。本研究表明,所提出的 QU-微乳具有在防晒配方中应用的良好潜力。