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Self‐Assembly Drug Delivery System Based on Programmable Dendritic Peptide Applied in Multidrug Resistance Tumor Therapy
Author(s) -
Chen Si,
Fan JinXuan,
Qiu WenXiu,
Liu LiHan,
Cheng Han,
Liu Fan,
Yan GuoPing,
Zhang XianZheng
Publication year - 2017
Publication title -
macromolecular rapid communications
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.348
H-Index - 154
eISSN - 1521-3927
pISSN - 1022-1336
DOI - 10.1002/marc.201700490
Subject(s) - multiple drug resistance , peptide , micelle , drug delivery , drug , in vivo , amphiphile , drug resistance , in vitro , rational design , chemistry , drug design , pharmacology , biophysics , materials science , combinatorial chemistry , biochemistry , nanotechnology , biology , organic chemistry , polymer , microbiology and biotechnology , aqueous solution , copolymer , antibiotics
In recent decades, diverse drug delivery systems (DDS) constructed by self‐assembly of dendritic peptides have shown advantages and improvable potential for cancer treatment. Here, an arginine‐enriched dendritic amphiphilic chimeric peptide CRRK(RRCG(Fmoc)) 2 containing multiple thiol groups is programmed to form drug‐loaded nano‐micelles by self‐assembly. With a rational design, the branched hydrophobic groups (Fmoc) of the peptides provide a strong hydrophobic force to prevent the drug from premature release, and the reduction‐sensitive disulfide linkages formed between contiguous peptides can control drug release under reducing stimulation. As expected, specific to multidrug resistance (MDR) tumor cells, the arginine‐enriched peptide/drug (PD) nano‐micelles show accurate nuclear localization ability to prevent the drug being pumped by P‐glycoprotein (P‐gp) in vitro, as well as exhibiting satisfactory efficacy for MDR tumor treatment in vivo. This design successfully realizes stimuli‐responsive drug release aimed at MDR tumor cells via an ingenious sequence arrangement.