Carbon Dots with Guanidinium and Amino Acid Functional Groups for Targeted Small Interfering RNA Delivery toward Tumor Gene Therapy.

Huimin Xu, Jianqiao Chang, Hao Wu, Haoyu Wang, Wenjing Xie, Yunchao Li, Xiaohong Li, Yang Zhang, Louzhen Fan

Small (Weinheim an der Bergstrasse, Germany) 2023 Aug

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Small interfering RNA (siRNA)-based gene therapy represents a promising strategy for tumor treatment. Novel gene vectors that can achieve targeted delivery of siRNA to the tumor cells without causing any side effects are urgently needed. To this end, the large amino acid mimicking carbon dots with guanidinium functionalization (LAAM GUA-CDs) are designed and synthesized by choosing arginine and dopamine hydrochloride as precursors. LAAM GUA-CDs can load siRNA through the multiple hydrogen bonds between their guanidinium groups and phosphate groups in siRNA. Meanwhile, the amino acid groups at the edges of LAAM GUA-CDs endow them the capacity to target tumors. After loading siBcl-2 as a therapeutic agent, LAAM GUA-CDs/siBcl-2 has a high tumor inhibition rate of up to 68%, which is twice more than that of commercial Lipofectamine 2000. Furthermore, LAAM GUA-CDs do not cause side effect during antitumor treatment owing to their high tumor-targeting ability, thus providing a versatile strategy for tumor-targeted siRNA delivery and cancer therapy. © 2023 Wiley-VCH GmbH.

Citation

Huimin Xu, Jianqiao Chang, Hao Wu, Haoyu Wang, Wenjing Xie, Yunchao Li, Xiaohong Li, Yang Zhang, Louzhen Fan. Carbon Dots with Guanidinium and Amino Acid Functional Groups for Targeted Small Interfering RNA Delivery toward Tumor Gene Therapy. Small (Weinheim an der Bergstrasse, Germany). 2023 Aug;19(31):e2207204