Biochemical Laboratory, Saraya Co. Ltd., 24-12 Tamate, Kashiwara, Osaka 582-0028, Japan.
Biochem Cell Biol. 2012 Jun;90(3):504-12. doi: 10.1139/o11-065. Epub 2012 Feb 14.
Lactoferrin (Lf), a multifunctional glycoprotein, is known to activate dermal fibroblasts. Enhancing percutaneous absorption without decreasing the activity of Lf is critical in making the dermal administration of Lf beneficial. Sophorolipid (SL), a glycolipid-type biosurfactant, is known to form assemblies that may elevate the efficiency of the transdermal delivery of active ingredients. Here, we investigated the role of SL in the transdermal absorption of bovine Lf (bLf) and the effect of SL on the bLf activity on dermal fibroblasts. Transdermal absorption of bLf through a model skin was enhanced by 1.3-fold to 1.7-fold when SL was added. The effects of SL on the bLf activities on dermal fibroblasts were examined by cell proliferation activities and by gene expression levels of elastic fiber components, collagen IV, and hyaluronan synthases, revealing that SL did not depress the effect of bLf to any extent. Instead, the tropoelastin gene expression was upregulated ~60-fold by bLf alone, which was further increased to ~160-fold by bLf and SL together, suggesting a significant synergism between bLf and SL. Protein levels of elastin, assessed by immunohistochemistry, correlated well with the results of gene expressions. These results indicate the feasibility of the transdermal administration of bLf with SL.
乳铁蛋白（Lf）是一种多功能糖蛋白，已知能激活真皮成纤维细胞。在使 Lf 经皮给药有益的情况下，提高经皮吸收而不降低 Lf 活性至关重要。槐糖脂（SL）是一种糖脂型生物表面活性剂，已知能形成组装体，可能会提高活性成分经皮传递的效率。在这里，我们研究了 SL 在牛乳铁蛋白（bLf）经皮吸收中的作用以及 SL 对真皮成纤维细胞中 bLf 活性的影响。当添加 SL 时，bLf 通过模型皮肤的经皮吸收增加了 1.3 倍至 1.7 倍。通过细胞增殖活性和弹性纤维成分、IV 型胶原和透明质酸合酶的基因表达水平检查了 SL 对 bLf 对真皮成纤维细胞活性的影响，结果表明 SL 并没有在任何程度上抑制 bLf 的作用。相反，bLf 单独将弹蛋白原基因表达上调约 60 倍，而 bLf 和 SL 一起进一步上调至约 160 倍，表明 bLf 和 SL 之间存在显著协同作用。通过免疫组织化学评估的弹性蛋白蛋白水平与基因表达结果非常吻合。这些结果表明了 bLf 与 SL 联合经皮给药的可行性。
