Casiraghi Antonella, Franzè Silvia, Selmin Francesca, Dazio Valeria, Minghetti Paola
Department of Pharmaceutical Sciences, University of Milan, Milan, Italy.
Humana Pharma International SpA, Milan, Italy.
Planta Med. 2017 Mar;83(5):405-411. doi: 10.1055/s-0042-108732. Epub 2016 Jun 10.
Epigallocatechin gallate, one of the most active antioxidant compounds, has a low chemical stability and ability to permeate the human epidermis. The encapsulation in polymeric micelles would be beneficial to improve both stability and permeation of epigallocatechin gallate and, therefore, to facilitate the pharmacological effects. Polymeric micelles containing epigallocatechin gallate were incorporated in O/W emulsions prepared by using different types of emulsifying systems. All emulsions were uniform in colour and aspect, without evidences of phase separation after centrifugation at the preparation time and over a 6-month period of storage at room temperature. Emulsions containing epigallocatechin gallate incorporated in polymeric micelles showed a colour variation, probably due to epigallocatechin gallate degradation, over the stability period. The skin permeability study evidenced a significant increase in epigallocatechin gallate permeation after encapsulation in micelles. Pure epigallocatechin gallate was not able to permeate the skin and only limited amounts were retained in the epidermis, while both permeated and retained amounts after 24 h were measured in the case of polymeric micelles containing epigallocatechin gallate. Moreover, the epigallocatechin gallate release and human skin permeability were affected by the type of emulsifier. The epigallocatechin gallate release in the presence of an emulsifier system based on cereal and fruit fibres never occurred. The best results in terms of release and skin permeability were obtained using glycerides of synthetic or semisynthetic origin or esters.
表没食子儿茶素没食子酸酯是最具活性的抗氧化化合物之一,其化学稳定性较低,且穿透人体表皮的能力有限。将其包裹于聚合物胶束中有利于提高表没食子儿茶素没食子酸酯的稳定性和渗透性,从而促进其药理作用。将含有表没食子儿茶素没食子酸酯的聚合物胶束加入到使用不同类型乳化体系制备的水包油乳液中。所有乳液在色泽和外观上均一,在制备时离心后以及在室温下储存6个月期间均未出现相分离迹象。在储存期内,含有包裹于聚合物胶束中的表没食子儿茶素没食子酸酯的乳液出现了颜色变化,这可能是由于表没食子儿茶素没食子酸酯降解所致。皮肤渗透性研究表明,表没食子儿茶素没食子酸酯包裹于胶束后其渗透性显著增加。纯表没食子儿茶素没食子酸酯无法穿透皮肤,仅在表皮中保留了有限的量,而对于含有表没食子儿茶素没食子酸酯的聚合物胶束,则测定了24小时后的渗透量和保留量。此外,表没食子儿茶素没食子酸酯的释放和人体皮肤渗透性受乳化剂类型的影响。在基于谷物和水果纤维的乳化体系存在下,表没食子儿茶素没食子酸酯不会释放。在释放和皮肤渗透性方面,使用合成或半合成来源的甘油酯或酯可获得最佳结果。