Surini Silvia, Leonyza Astried, Suh Chang Woo
Laboratory of Pharmaceutics and Pharmaceutical Technology Development, Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, 16424, Indonesia.
PT Daewoong Pharmaceutical Company Indonesia, Jakarta 10230, Indonesia.
Adv Pharm Bull. 2020 Sep;10(4):586-594. doi: 10.34172/apb.2020.070. Epub 2020 Aug 9.
Recombinant human epidermal growth factor (rhEGF) is a 6045-Da peptide that promotes the cell growth process, and it is also used for cosmetic purposes as an anti-aging compound. However, its penetration into skin is limited by its large molecular size. This study aimed to prepare rhEGF-loaded transfersomal emulgel with enhanced skin penetration compared with that of non-transfersomal rhEGF emulgel. Three transfersome formulations were prepared with different ratios between the lipid vesicle (phospholipid and surfactant) and rhEGF (200:1, 133:1, and 100:1) using a thin-film hydration-extrusion method. The physicochemical properties of these transfersomes and the percutaneous delivery of the transfersomal emulgel were evaluated. Long-term and accelerated stability studies were also conducted. The 200:1 ratio of lipid to drug was optimal for rhEGF-loaded transfersomes, which had a particle size of 128.1 ± 0.66 nm, polydispersity index of 0.109 ± 0.004, zeta potential of -43.1 ± 1.07 mV, deformability index of 1.254 ± 0.02, and entrapment efficiency of 97.77% ± 0.09%. Transmission electron microscopy revealed that the transfersomes had spherical and unilamellar vesicles. The skin penetration of rhEGF was enhanced by as much as 5.56 fold by transfersomal emulgel compared with that of non-transfersomal emulgel. The stability study illustrated that the rhEGF levels after 3 months were 84.96-105.73 and 54.45%-66.13% at storage conditions of 2°C-8°C and 25°C ± 2°C/RH 60% ± 5%, respectively. The emulgel preparation containing transfersomes enhanced rhEGF penetration into the skin, and skin penetration was improved by increasing the lipid content.
重组人表皮生长因子（rhEGF）是一种6045道尔顿的肽，可促进细胞生长过程，还作为抗衰老化合物用于美容目的。然而，其大分子尺寸限制了它渗透进入皮肤。本研究旨在制备负载rhEGF的传递体乳化凝胶，与非传递体rhEGF乳化凝胶相比，增强其皮肤渗透性。使用薄膜水化-挤压法，制备了脂质囊泡（磷脂和表面活性剂）与rhEGF比例不同（200:1、133:1和100:1）的三种传递体制剂。评估了这些传递体的物理化学性质以及传递体乳化凝胶的经皮递送情况。还进行了长期和加速稳定性研究。脂质与药物比例为200:1时，对负载rhEGF的传递体最为适宜，其粒径为128.1±0.66纳米，多分散指数为0.109±0.004，ζ电位为-43.1±1.07毫伏，变形性指数为1.254±0.02，包封率为97.77%±0.09%。透射电子显微镜显示传递体为球形单室囊泡。与非传递体乳化凝胶相比，传递体乳化凝胶使rhEGF的皮肤渗透性提高了5.56倍。稳定性研究表明，在2℃-8℃和25℃±2℃/相对湿度60%±5%的储存条件下，3个月后rhEGF水平分别为84.96 - 105.73和54.45% - 66.13%。含有传递体的乳化凝胶制剂增强了rhEGF渗透进入皮肤的能力，并且通过增加脂质含量改善了皮肤渗透性。
