Synthesis and characterization of a carbon nanotube-dendron series for efficient siRNA delivery.
A new series of dendron-functionalized multiwalled carbon nanotube (MWNT) derivatives, characterized by the presence of numerous positively charged tetraalkyl ammonium salts at the periphery of the dendron, has been synthesized. The positive charges on the MWNT surface, coupled with the unique ability of carbon nanotubes (CNTs) to penetrate cell membranes, make the new derivatives potentially ideal vectors for siRNA delivery. Using a fluorescently labeled, noncoding siRNA sequence, we demonstrate that cytoplasmic delivery of the nucleic acid is remarkably increased throughout the different dendron generations. The work reported here highlights the fact that dendron-functionalized CNTs can be rationally designed as efficient carriers of siRNA that can eventually lead to gene silencing.
Herrero
M Antonia
MA
Center of Excellence for Nanostructured Materials, Department of Pharmaceutical Sciences, and INSTM, University of Trieste, Piazzale Europa 1, 34127 Trieste, Italy.
Toma
Francesca M
FM
Al-Jamal
Khuloud T
KT
Kostarelos
Kostas
K
Bianco
Alberto
A
Da Ros
Tatiana
T
Bano
Fouzia
F
Casalis
Loredana
L
Scoles
Giacinto
G
Prato
Maurizio
M
D000179:Acrylates / Q000737:chemistry; D000818:Animals; D001391:Azo Compounds / Q000737:chemistry; D001692:Biological Transport; D003593:Cytoplasm / Q000378:metabolism; D050091:Dendrimers; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry*; D005029:Ethylenediamines / Q000737:chemistry; D020868:Gene Silencing; D006367:HeLa Cells; D006801:Humans; D037742:Nanotubes, Carbon / Q000737:chemistry*; D011073:Polyamines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D034741:RNA, Small Interfering / Q000235:genetics / Q000378:metabolism*; D012995:Solubility; D013882:Thiosemicarbazones / Q000737:chemistry; D014162:Transfection; D014867:Water / Q000737:chemistry
D000179:Acrylates; D001391:Azo Compounds; D050091:Dendrimers; D004337:Drug Carriers; D005029:Ethylenediamines; D037742:Nanotubes, Carbon; C104700:PAMAM Starburst; D011073:Polyamines; D034741:RNA, Small Interfering; D013882:Thiosemicarbazones; C512188:azomethine; D014867:Water; C031234:ethylenediamine; C035956:methyl acrylate