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. 2015 Jan 17;20(6):750–759. doi: 10.1016/j.drudis.2015.01.006

Table 1.

Various bioactives delivered through functionalized CNTs for pharmaceutical and biomedical applications

Functionalized CNTs Cell lines used Bioactives agents used Physicochemical/biological parameters Outcomes of the study References
FITC-MWCNTs & Oxidized MWCNTs Human Jurkat T lymphoma cells Amphotericin B (AmB) via covalent attachment Electron microscopy
Antifungal activity
AmB covalently linked to CNTs is taken up by mammalian cells devoid any specific toxic effect. f-CNTs are able to enter the cell by a spontaneous mechanism. [34]
PL-PEG-FA & PL-PEG-FITC-SWCNTs. HeLa cells Cy3-labeled DNA Atomic force microscopy
Confocal laser scanning microscopy
SWCNTs internalized in living cells can act as tiny NIR ‘heaters’ or ‘antennas’. [10]
PL-PEG-RGD-SWCNT & FITC annexin V-SWCNTs. MCF-7 breast cancer and U87 MG cancer cell lines Doxorubicin Fluorescence
Supramolecular loading efficiency
Enhanced uptake of DOX in case of integrin-positive U87 MG using RGD-based targeting relative to integrin-negative MCF-7 Cells. [40]
PL-PEG-SWCNTs NTera-2 Cisplatin prodrug conjugate Fluorescence microscopy Cytotoxicity of the free platinum(IV) complex increases by >100-fold when the complex is attached to the surface of the functionalized SWNTs. [41]
Pluronic F 127 stabilized-MWCNTs MCF-7 human breast cancer cells Doxorubicin through π–π stacking Electron microscopy
Confocal laser microscopy
Enhanced cytotoxicity of DOX-MWCNTs complex over free DOX. [42]
DSPE-PEG5000-PTX-SWCNTs
PEG- SWCNTs.
4T1 tumor-bearing mice (tumor size, ∼200 mm3). Paclitaxel (PTX) Pharmacokinetics and biodistribution study
Antitumor efficacy
Pilot toxicity study
Water-soluble SWCNTs-PTX formulation is cremophor-free.
SWCNTs have shown to be safe at least in mouse models.
[43]
CNTs Bladder cancer cells Carboplatin Electron energy loss spectroscopy
X-ray-photoelectron spectroscopy
Cell proliferation
Cytotoxicity
High efficacy of carboplatin filled CNTs with reduced growth of bladder cancer cells compared to free drug CNTs. [44]
Folic acid (FA)-chitosan (CHI)/alginate (ALG)-SWCNTs. HeLa cell line Doxorubicin through π–π stacking. Fluorescence
Cell viability and cell uptake studies
CNTs complex found to be more selective and effective than free DOX due to targeting based on FA and release of DOX at lysosomal pH. [45]
mAB-BSA adsorbed-SWCNTs. WPDr colon cancer cell line Doxorubicin through π–π stacking. Electron microscopy (SEM, HRTEM)
Raman spectroscopy
Uptake study revealed that delivery efficiency was 100%.
All cells could take up the SWCNT complexes.
[46]
Diaminotriethylene glycol-MWCNTs. MKN-28 cells and H22 cell lines 10-Hydroxycamptothecin (HCPT) through π–π stacking. In vitro single photon emission computed tomography (SPECT).
ex vivo gamma scintillation counting analysis
MWCNTs-HCPT conjugate enhanced superior antitumor activity both in vitro and in vivo to clinical HCPT formulation. They show relatively long blood circulation and high drug accumulation at the tumor site. [47]
Dapsone-MWCNTs-FITC Subvert normal macrophage (MØ) and PMØ Dapsone (DDS) Confocal laser microscopy
Phagocytosis assay
Dapsone-MWCNTs did not trigger oxidative stress but caused apoptosis of PMØ predominantly after prolonged cultivation (3 days). [48]
Azomethine ylide (1.3-dipolar cycloaddition)-MWCNTs. MCF-7 Cell line. Methotrexate (MTX) through cleavable ester bond. Electron microscopy
Cytotoxicity study
Cytotoxic activity of CNTs conjugate was strongly dependent on the presence and type of linker. [49]
EGF-SWCNTs–cisplatin–EGF Head and Neck Squamous Carcinoma Cells
(HNSCC), HN12 cells
Cisplatin Histological analysis
Raman analysis
Annexin V assay
PEG-SWCNTs, as opposed to control SWCNTs, form more highly dispersed delivery vehicles that, when loaded with both cisplatin and EGF, inhibit growth of squamous cell tumors. [50]
Sgc8c aptamer-SWCNTs Molt-4 (Target) and U266 non-target (B lymphocyte human myeloma) cell line Daunorubicin (anthracycline antibiotic) through π–π stacking Cell viability
Loading efficiency ∼157%
Flow cytometry analysis
Dau-aptamer-SWCNTs complex was able to selectively target Molt-4 cells compared to non target cells. [51]
CNT-PEI and CNT-pyridinium-MWCNTs Human lung cancer cells (H1299) siRNA Gene silencing and cytotoxicity agarose gel electrophoresis CNT-PEI and CNT-pyridinium did not show any added value over PEI, pDMAEMA, and Lipofectamine used as reference transfection agents for siRNA silencing activity and cytotoxicity. [52]
Hyaluronate tethered MWCNTs A 549 cell line Doxorubicin (DOX) Pharmacodynamic and organ distribution studies
Tumor growth inhibition studies
Apoptosis study
Cytotoxicity study
The 99mTc-MWCNT-HA-DOX is significantly higher than both free drug and non-targeted MWCNTs in organ distribution studies on Ehlrich ascites tumor (EAT) bearing mice.
The tumor-growth inhibitory effect of HA-MWCNTs-DOX was found to be 5 times higher than free DOX in chemically breast-cancer-induced model in pharmacodynamic studies devoid of any detectable cardiotoxity, hepatotoxicity, or nephrotoxicity.
[53]
DOX-FA-MN-MWCNT U87 cell lines Doxorubicin Electron microscopy
CLSM.
Dual targeted DOX-FA-MN-MWCNTs showed the high drug loading, pH-dependent controlled release, magnetic targeting, and ligand–receptor interactions. [37]
AmB/Mannose-MWCNTs J774 cells Amphotericin B (AmB) CLSM
In vitro & in vivo studies
macrophage uptake study
AmBitubes showed better targeting efficiency to macrophages i.e. J 774 cell lines with reduced toxic effects associated with AmB. [36]
DOX/DEX-MWCNTs A-549 cells Doxorubicin (DOX) In vitro & ex vivo studies DOX/DEX-MWCNTs found less hemolytic and more cytotoxic as compared to free DOX on A-549 lung epithelial cancer cell line. [38]
Functionalized MWCNTs Raw 264.7 and A-549 cell lines Immunofluorescence microscopy The chemical functionalization tailors the fate of CNTs by tilting the balance toward specific mechanisms of internalization, cellular processing and elimination/degradation. [13]
Angiopeptide conjugated PEGylated oxidized MWCNTs Brain capillary endothelial cells (BCEC) and C6 glioma cells Doxorubicin (DOX) Anti-glioma efficacy
Intracellular fluorescence distribution.
Fluorescence imaging
The results showed that DOX-O-MWCNTs-PEG-ANG is a promising dual-targeting carrier to deliver DOX for the treatment of brain tumor [22]
f-SWCNTs-COS-GTX-p53 HeLa and MCF-7 cells Gliotoxin Cytotoxicity study
Fluorescent activated cell sorter analysis
The f-SWCNTs-COS-GTX-p53 was found to be most effective delivery vehicle with a controlled release and enhanced cytotoxicity rendered through apoptosis in HeLa cells. [54]
GL-MWCNTs-DOX HepG2 cell Doxorubicin Electron microscopy
Flow cytometry and phase contrast microscopy
Anticancer activity
GL-MWCNTs-DOX formulation approach was found to be promising toward development of an affluent liver targeting. [55]

MWCNTs: Multi walled carbon nanotubes; SWCNTs: Single walled carbon nanotubes; FITC: Fluorescence isothiocynate; PEI: Polyethyleneimine; PL-PEG: Phoshpholipid-Polyethlene glycol; RGD: Arginine-glycine-aspartic acid; NGR: Asn-Gly-Arg; HCPT: Hydroxycamptothecin; NIR: Near infrared; EGF: Epidermal growth factor; PL-PEG-FA: Phospholipid polyethylene glycol-folic acid; PEI: Polyethleneimine; siRNA: small interfering ribonucleic acid; Amphotericin B: AmB; GTX: Gliotoxin; GL: Glycyrrhizinic acid; DOX: Doxorubicin.