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Spherical Nucleic Acids for Topical Treatment of Hyperpigmentation.


ABSTRACT: 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.

SUBMITTER: Fang Y 

PROVIDER: S-EPMC8313479 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature

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Spherical Nucleic Acids for Topical Treatment of Hyperpigmentation.

Fang Yang Y   Lu Xueguang X   Wang Dali D   Cai Jiansong J   Wang Yuyan Y   Chen Peiru P   Ren Mengqi M   Lu Hao H   Union Jennifer J   Zhang Lei L   Sun Yehui Y   Jia Fei F   Kang Xi X   Tan Xuyu X   Zhang Ke K  

Journal of the American Chemical Society 20210112 3


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  ...[more]

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