期刊
SMALL
卷 19, 期 31, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/smll.202207204
关键词
guanidinium functionalization; RNA interference therapeutic; small interfering RNA delivery; tumor gene therapy; tumor-targeted carbon dots
siRNA-based gene therapy is a promising strategy for tumor treatment. Novel gene vectors, such as LAAM GUA-CDs, which can target tumor cells and deliver siRNA without causing side effects, have been designed and synthesized. LAAM GUA-CDs loaded with siBcl-2 exhibit a high tumor inhibition rate, twice as effective as commercial Lipofectamine 2000. LAAM GUA-CDs provide a versatile approach for tumor-targeted siRNA delivery and cancer therapy.
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.
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