TY - JOUR
T1 - SiRNA delivery with functionalized carbon nanotubes
AU - Varkouhi, Amir Khashayar
AU - Foillard, Stéphanie
AU - Lammers, Twan
AU - Schiffelers, Raymond M.
AU - Doris, Eric
AU - Hennink, Wim E.
AU - Storm, Gert
PY - 2011/9/20
Y1 - 2011/9/20
N2 - Carbon nanotubes (CNTs) have been studied for drug, antigen and nucleic acid delivery both in vitro and in vivo. Due to their nano-needle structure, they are supposed to cross the plasma membrane and enter directly into the cytoplasm likely upon an endocytosis-independent mechanism without inducing cell death. In this study, two cationically functionalized CNTs (CNT-PEI and CNT-pyridinium) were investigated for siRNA delivery. Both functionalized CNTs complexed siRNA and showed 10-30% silencing activity and a cytotoxicity of 10-60%. However, in terms of reduced toxicity or increased silencing activity, CNT-PEI and CNT-pyridinium did not show an added value over PEI and other standard transfection systems. Probably, the type of functionalization of carbon nanotubes might be a key parameter to obtain an efficient and non-cytotoxic CNT-based delivery system. Nevertheless, in view of the present results and importantly also of the non-degradability of CNTs, preference should currently be given to designing biodegradable carriers which mimic the needle structure of CNTs.
AB - Carbon nanotubes (CNTs) have been studied for drug, antigen and nucleic acid delivery both in vitro and in vivo. Due to their nano-needle structure, they are supposed to cross the plasma membrane and enter directly into the cytoplasm likely upon an endocytosis-independent mechanism without inducing cell death. In this study, two cationically functionalized CNTs (CNT-PEI and CNT-pyridinium) were investigated for siRNA delivery. Both functionalized CNTs complexed siRNA and showed 10-30% silencing activity and a cytotoxicity of 10-60%. However, in terms of reduced toxicity or increased silencing activity, CNT-PEI and CNT-pyridinium did not show an added value over PEI and other standard transfection systems. Probably, the type of functionalization of carbon nanotubes might be a key parameter to obtain an efficient and non-cytotoxic CNT-based delivery system. Nevertheless, in view of the present results and importantly also of the non-degradability of CNTs, preference should currently be given to designing biodegradable carriers which mimic the needle structure of CNTs.
KW - Carbon nanotube
KW - Cytotoxicity
KW - Gene silencing
KW - SIRNA
UR - http://www.scopus.com/inward/record.url?scp=79961032439&partnerID=8YFLogxK
U2 - 10.1016/j.ijpharm.2011.02.009
DO - 10.1016/j.ijpharm.2011.02.009
M3 - Article
C2 - 21320582
AN - SCOPUS:79961032439
SN - 0378-5173
VL - 416
SP - 419
EP - 425
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
IS - 2
ER -