Dual targeting of a thermosensitive nanogel conjugated with transferrin and RGD-containing peptide for effective cell uptake and drug release.
In this paper, both arginine-glycine-aspartic acid (RGD)-containing peptide and transferrin (Tf) were conjugated to the thermosensitive poly(N-isopropylacrylamide-co-propyl acrylic acid) (poly(NIPAAm-co-PAAc)) nanogel to prepare a dual-targeting drug carrier. The obtained nanogel was characterized in terms of fluorescence spectroscopy, UV-vis spectroscopy, dynamic light scattering (DLS) and transmission electron microscopy (TEM). In order to track the dual-ligand conjugated nanogel, fluorescein isothiocyanate (FITC) was further conjugated to the nanogel. A cell internalization experiment showed that the dual-ligand conjugated nanogel exhibited obviously enhanced endocytosis by HeLa cells as compared with non-tumorous cells (COS-7 cells). The drug-loaded dual-ligand conjugated nanogel could be transported efficiently into the target tumor cells and the anti-tumor effect was enhanced significantly, suggesting that the dual-ligand conjugated nanogel has great potential as a tumor targeting drug carrier.
Quan
Chang-Yun
CY
Key Laboratory of Biomedical Polymers of Ministry of Education & Department of Chemistry, Wuhan University, Wuhan 430072, People's Republic of China.
Chang
Cong
C
Wei
Hua
H
Chen
Chang-Sheng
CS
Xu
Xiao-Ding
XD
Cheng
Si-Xue
SX
Zhang
Xian-Zheng
XZ
Zhuo
Ren-Xi
RX
D000178:Acrylamides; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D002021:Buffers; D019556:COS Cells; D016923:Cell Death / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D004317:Doxorubicin / Q000494:pharmacology*; D016503:Drug Delivery Systems; D004705:Endocytosis / Q000187:drug effects; D016650:Fluorescein-5-isothiocyanate / Q000378:metabolism; D006367:HeLa Cells; D006801:Humans; D018613:Microscopy, Confocal; D000080385:Nanogels; D009842:Oligopeptides / Q000737:chemistry / Q000378:metabolism*; D010455:Peptides / Q000737:chemistry / Q000378:metabolism*; D011092:Polyethylene Glycols / Q000737:chemistry*; D011094:Polyethyleneimine / Q000737:chemistry*; D012996:Solutions; D013050:Spectrometry, Fluorescence; D013056:Spectrophotometry, Ultraviolet; D013696:Temperature; D014168:Transferrin / Q000378:metabolism*
D000178:Acrylamides; D000970:Antineoplastic Agents; D002021:Buffers; D000080385:Nanogels; D009842:Oligopeptides; D010455:Peptides; D012996:Solutions; D014168:Transferrin; C512582:poly(N-isopropylacrylamide-co-propylacrylic acid); C413692:polyethylene glycol polyethyleneimine nanogel; D011092:Polyethylene Glycols; C047981:arginyl-glycyl-aspartic acid; D004317:Doxorubicin; D011094:Polyethyleneimine; D016650:Fluorescein-5-isothiocyanate