Cancer targeting propensity of folate conjugated surface engineered multi-walled carbon nanotubes

• CNTs comprise of thin graphite sheets of condensed benzene ring rolled upon into the nanoneedle, seamless tubular hollow cylinder.
• The DTX loaded FA PEGylated MWCNTs formulations arrest cell death in G2 phase.
• The in vivo pharmacokinetic studies described that highly functionalized MWCNTs formulations are long-circulating (stealth) in nature.
• The Kaplan–Meier survival curve analysis showed the median survival time for tumor bearing mice of DTX/FA-PEG-MWCNTs was significantly longer survival span (40 days, p < 0.001).
• The DTX/FA-PEG-MWCNTs holds strong targeting potential in cancer treatment.

Our main aim in the present investigation was to investigate the cancer targeting potential of docetaxel (DTX) loaded, folic acid (FA) terminated, poly (ethylene glycol) (PEG) conjugated, surface engineered multi walled carbon nanotubes (DTX/FA-PEG-MWCNTs) in tumor bearing Balb/c mice. The percent loading efficiency of DTX/FA-PEG-MWCNTs and DTX loaded MWCNTS (DTX/MWCNTs) was calculated to be 93.40 ± 3.82% and 76.30 ± 2.62%, respectively. Flow cytometry analysis suggested that the DTX/FA-PEG-MWCNTs arrested MCF-7 cells’ cycle in the G2 phase and was more cytotoxic as compared to DTX/MWCNTs as well as free drug solution. The obtained pharmacokinetic parameters clearly describe the biocompatibility of engineered nanotubes to degree of functionalization and ability for prolonged residence inside the body. DTX/FA-PEG-MWCNTs was found to be significantly more efficient in tumor suppression as compared with plain MWCNTs (non-targeted) as well as drug solution owing to the enhanced drug release from endosomes after internalization. The DTX/FA-PEG-MWCNTs showed highly significant prolonged survival span (40 days) as compared to DTX/MWCNTs (24 days), free DTX (19 days) and control group (12 days). Overall, we can conclude that the DTX/FA-PEG-MWCNTs shows higher cancer targeting propensity vis a vis minimal side effects in tumor bearing Balb/c mice.

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