Reductive nanocomplex encapsulation of cRGD-siRNA conjugates for enhanced targeting to cancer cells.

ABSTRACT: In this study, through covalent conjugation and lipid material entrapment, a combined modification strategy was established for effective delivery of small interfering RNA (siRNA). Single strands of siRNA targeting to BRAF^V600E gene (siMB3) conjugated with cRGD peptide at 3'-terminus or 5'-terminus via cleavable disulfide bond was synthesized and then annealed with corresponding strands to obtain single and bis-cRGD-siRNA conjugates. A cationic lipid material (CLD) developed by our laboratory was mixed with the conjugates to generate nanocomplexes; their uniformity and electrical property were revealed by particle size and zeta potential measurement. Compared with CLD/siBraf, CLD/cRGD-siBraf achieved higher cell uptake and more excellent tumor-targeting ability, especiall

SUBMITTER: Zhou Z 

PROVIDER: S-EPMC5634379 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature