Poomanee Worrapan, Chaiyana Wantida, Randall Wickett R, Leelapornpisid Pimporn
Faculty of Pharmacy, Chiang Mai University, Chiang Mai, Thailand.
James L. Winkle College of Pharmacy, University of Cincinnati, Cincinnati, USA.
Asian J Pharm Sci. 2017 Jul;12(4):386-393. doi: 10.1016/j.ajps.2017.03.001. Epub 2017 Mar 8.
The aim of this study was to enhance the solubility and stability of extract by loading in a microemulsion for topical application. Both physical appearance and biological activities of the extract-loaded microemulsion were determined in comparison with the extract solution. Pseudoternary phase diagrams of three oil types including tea seed oil, grape seed oil, and sesame oil, together with polysorbate 85 or the mixture of polysorbate 85 and sorbitan oleate as surfactants, and absolute ethanol as a co-surfactant were constructed to optimize the microemulsion area. The selected microemulsion was then characterized for droplet size, polydispersity index, and viscosity. Tea seed oil exhibited the highest microemulsion area in the phase diagram because it had the highest unsaturated fatty acid content. The microemulsion composed of tea seed oil (5%), polysorbate 85 (40%), ethanol (20%), and water (35%) exhibited Newtonian flow behavior with the droplet size and polydispersity index of 68.03 ± 1.09 nm and 0.44 ± 0.04, respectively. After 4% w/w of the extract was incorporated into the microemulsion, larger droplets size was observed (239.77 ± 12.69 nm) with a lower polydispersity index (0.37 ± 0.02). After storage in various conditions, both physical appearances and the stability of biological activity of the extract-loaded microemulsion were improved compared to the solution. Therefore, the loaded microemulsion may be a promising carrier for further development into a topical formulation and clinical trials for pharmaceutical and cosmeceutical applications are also suggested.
本研究的目的是通过将提取物负载于微乳中用于局部应用,以提高其溶解度和稳定性。将负载提取物的微乳的物理外观和生物活性与提取物溶液进行比较测定。构建了三种油类(茶籽油、葡萄籽油和芝麻油)的拟三元相图,以聚山梨酯85或聚山梨酯85与脱水山梨醇油酸酯的混合物为表面活性剂,无水乙醇为助表面活性剂,以优化微乳区域。然后对所选微乳的粒径、多分散指数和粘度进行表征。茶籽油在相图中显示出最大的微乳区域,因为其不饱和脂肪酸含量最高。由茶籽油(5%)、聚山梨酯85(40%)、乙醇(20%)和水(35%)组成的微乳表现出牛顿流体行为,其粒径和多分散指数分别为68.03±1.09nm和0.44±0.04。将4%w/w的提取物加入微乳后,观察到粒径增大(239.77±12.69nm),多分散指数降低(0.37±0.02)。在各种条件下储存后,与溶液相比,负载提取物的微乳的物理外观和生物活性稳定性均得到改善。因此,负载微乳可能是一种有前途的载体,有望进一步开发成局部制剂,也建议进行用于药物和药妆应用的临床试验。