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Development of Polymeric Micelles of Oleanolic Acid and Evaluation of Their Clinical Efficacy.
Nanoscale Research Letters ( IF 5.5 ) Pub Date : 2020-06-22 , DOI: 10.1186/s11671-020-03348-3
Joo Young An 1, 2 , Hee Seon Yang 1, 3 , Na Rae Park 1, 3 , Tae-Sung Koo 3 , Bungchul Shin 1 , Eun Hee Lee 2 , Sun Hang Cho 1
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Oleanolic acid has been used only as a subsidiary agent in cosmetic products. The aim of the study is to show the effect of oleanolic acid as an active ingredient for the alleviation of wrinkles in humans and to develop a polymeric micelle formulation that enables poorly soluble oleanolic acid to be used as a main ingredient in cosmetic products for reducing wrinkles. The solubility of oleanolic acid was evaluated in solubilizers, surfactants, and polymers. The particle sizes and shapes of polymeric micelles containing oleanolic acid were evaluated by electrophoretic light scattering spectrophotometer and scanning electron cryomicroscopy. Encapsulation efficiency and skin permeation were measured by HPLC. Stability of the polymeric micelles stored at 40 °C for 3 months was evaluated by visual observation, particle size measurement, and oleanolic acid content measurement. Polymeric micelles in final product ampoule form were applied around the eyes of 23 female subjects for 8 weeks. Five skin parameters were evaluated by optical profilometry every 4 weeks for 8 weeks. In addition, professionals made visual observations of the skin and a human skin irritation study was conducted. Polymeric micelles of oleanolic acid with a particle size of less than 100 nm were prepared using Capryol 90® and poloxamer. The skin permeation rate of the oleanolic acid in the polymeric micelles was higher than that in the other solutions made of oleanolic acid dispersed in 2 different surfactants. No significant changes in particle size, color, or oleanolic acid content were observed, and the polymeric micelles stored at 40 °C for 3 months did not undergo phase separation. After 8 weeks of application, skin irritation had not developed and all five parameters evaluated by optical profilometry as well as the visual evaluation scores were significantly improved. This study showed that the polymeric micelles of oleanolic acid prepared in this study were stable and effective at alleviating wrinkles in humans as the principal active ingredient. Based on these findings, it is expected that polymeric micelles of oleanolic acid can be widely used in cosmetic applications.



中文翻译:

齐墩果酸聚合物胶束的开发及其临床疗效评价。

齐墩果酸仅用作化妆品中的辅助剂。该研究的目的是显示齐墩果酸作为缓解人类皱纹的有效成分的作用,并开发出一种聚合物胶束配方,该配方可将难溶性齐墩果酸用作化妆品中减少皱纹的主要成分。评价齐墩果酸在增溶剂,表面活性剂和聚合物中的溶解度。通过电泳光散射分光光度计和扫描电子低温显微镜评价含有齐墩果酸的聚合物胶束的粒径和形状。通过HPLC测量包封效率和皮肤渗透。通过视觉观察,粒度测量,在40℃下储存3个月的聚合物胶束的稳定性,和齐墩果酸含量的测量。将最终产品安瓿形式的聚合物胶束涂在23名女性受试者的眼睛周围8周。每8周通过光学轮廓测量法评估5种皮肤参数。此外,专业人员对皮肤进行了视觉观察,并进行了人体皮肤刺激研究。使用Capryol90®和泊洛沙姆制备粒径小于100 nm的齐墩果酸聚合物胶束。聚合物胶束中齐墩果酸的皮肤渗透率高于由齐墩果酸分散在两种不同表面活性剂中制成的其他溶液中的皮肤渗透率。没有观察到粒径,颜色或齐墩果酸含量的显着变化,并且在40℃下储存3个月的聚合物胶束未经历相分离。施用8周后,仍未出现皮肤刺激,并且通过光学轮廓仪评估的所有五个参数以及视觉评估得分均得到显着改善。这项研究表明,这项研究中制备的齐墩果酸聚合物胶束是稳定有效的,可减轻人体内作为主要活性成分的皱纹。基于这些发现,预期齐墩果酸的聚合胶束可广泛用于化妆品应用中。

更新日期:2020-06-22
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