화학공학소재연구정보센터
학회 한국공업화학회
학술대회 2021년 봄 (05/12 ~ 05/14, 부산 벡스코(BEXCO))
권호 25권 1호
발표분야 포스터-생체재료
제목 Systemic siRNA Delivery with Redox-responsive Bile Acid-Modified Polyethylenimine Nanoparticles in Cancer Therapy
초록 Small interfering RNA (siRNA) delivery has been considered as a potential cancer therapy because it contributes to RNA interference (RNAi) by inhibiting target gene expression in a sequence-specific manner. In this study, low molecular weight polyethylnimine (PEI, 1.8 kDa) was conjugated with deoxycholic acid (DA). A DA-PEI conjugate was further modified with 4-fluorothiophenol (FTP) (TP-DA-PEI) to enhance systemic siRNA delivery. The thiophenol group would be involved with disulfide bonds between the polymer chains and siRNA modified with free thiols (thiol-siRNA) to form and π-π interactions between the pendent aromatic groups and coprostane ring of the bile acid. The stabilized TP-DA-PEI conjugate with thiol-siRNA achieved enhanced intracellular uptake, serum stability, and transfection efficiency. In addition, it showed high accumulation of TP-DA-PEI/thiol-siRNA polyplexes and significant tumor growth inhibition effect in tumor-bearing mice after systemic administration.
저자 김다훤, 임수연, LYUSIYAN, 황위보, 박채은, 김병덕, 정지훈
소속 성균관대
키워드 gene therapy; deoxycholic acid; disulfide crosslinking
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