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A Fluorinated Bola‐Amphiphilic Dendrimer for On‐Demand Delivery of siRNA, via Specific Response to Reactive Oxygen Species
Author(s) -
Liu Xiaoxuan,
Wang Yang,
Chen Chao,
Tintaru Aura,
Cao Yu,
Liu Juan,
Ziarelli Fabio,
Tang Jingjie,
Guo Hongbo,
Rosas Roseline,
Giorgio Suzanne,
Charles Laurence,
Rocchi Palma,
Peng Ling
Publication year - 2016
Publication title -
advanced functional materials
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 6.069
H-Index - 322
eISSN - 1616-3028
pISSN - 1616-301X
DOI - 10.1002/adfm.201604192
Subject(s) - dendrimer , amphiphile , reactive oxygen species , small interfering rna , drug delivery , biophysics , gene delivery , materials science , gene silencing , nanotechnology , chemistry , biochemistry , rna , transfection , biology , gene , polymer , copolymer , composite material
Functional materials capable of responding to stimuli intrinsic to diseases are extremely important for specific drug delivery at the disease site. However, developing on‐demand stimulus‐responsive vectors for targeted delivery is highly challenging. Here, a stimulus‐responsive fluorinated bola‐amphiphilic dendrimer is reported for on‐demand delivery of small interfering RNA (siRNA) in response to the characteristic high level of reactive oxygen species (ROS) in cancer cells. This dendrimer bears a ROS‐sensitive thioacetal in the hydrophobic core and positively charged poly(amidoamine) dendrons at the terminals, capable of interacting and compacting the negatively charged siRNA into nanoparticles to protect the siRNA and promote cellular uptake. The ROS‐sensitive feature of this dendrimer boosts specific and efficient disassembly of the siRNA/vector complexes in ROS‐rich cancer cells for effective siRNA delivery and gene silencing. Moreover, the fluorine tags in the vector enable 19 F‐NMR analysis of the ROS‐responsive delivery process. In addition, this ingenious and distinct bola‐amphiphilic dendrimer is also able to combine the advantageous delivery features of both lipid and dendrimer vectors. Therefore, it represents an innovative on‐demand stimulus‐responsive delivery platform.