Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
Department of Chemistry, Massachusetts Institute of Technology, 77 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.
J Am Chem Soc. 2021 Jan 27;143(3):1296-1300. doi: 10.1021/jacs.0c12044. Epub 2021 Jan 12.
Oligonucleotide-based materials such as spherical nucleic acid (SNA) have been reported to exhibit improved penetration through the epidermis and the dermis of the skin upon topical application. Herein, we report a self-assembled, skin-depigmenting SNA structure, which is based upon a bifunctional oligonucleotide amphiphile containing an antisense oligonucleotide and a tyrosinase inhibitor prodrug. The two components work synergistically to increase oligonucleotide cellular uptake, enhance drug solubility, and promote skin penetration. The particles were shown to reduce melanin content in B16F10 melanoma cells and exhibited a potent antimelanogenic effect in an ultraviolet B-induced hyperpigmentation mouse model.
基于寡核苷酸的材料，如球形核酸（SNA），据报道，在局部应用时能提高穿透表皮和真皮的能力。在此，我们报告了一种自组装的、皮肤美白的 SNA 结构，它基于一种双功能寡核苷酸两亲物，含有反义寡核苷酸和酪氨酸酶抑制剂前药。这两个组件协同作用，增加了寡核苷酸的细胞摄取，提高了药物的溶解度，并促进了皮肤渗透。这些颗粒被证明可以减少 B16F10 黑色素瘤细胞中的黑色素含量，并在紫外线 B 诱导的色素沉着过度的小鼠模型中表现出很强的美白效果。
