Table 3.
List of TKI-nanoconstruct applications published recently
| Nanomaterial | TKI | Effect | Targeting | Targeting ligand | Ref. |
|---|---|---|---|---|---|
| Gold NPs | Afatinib | Improvement of efficacy and biocompatibility | Passive | - | 86 |
| Immunoliposomes | Afatinib Cetuximab |
Protection from binding to hemoglobin, strongly enhanced drug delivery and anti-tumor efficacy, selectivity and potentially fewer side effects. | Active | Anti-EGFR antibody | 80 |
| Liposomes | Afatinib | Improved anti-tumor activity | Passive | - | 166 |
| Colloidal polyethylene glycolated (PEG) gold NPs | Afatinib | Higher cellular uptake, 5 and 20 times more potent than Afatinib alone | Passive | - | 167 |
| Cyclic arginylglycylaspartic acid (cRGD) and PEG-modified liposomes | Apatinib | Significant tumor treatment targeting ability, better inhibition of tumor growth, and less toxicity. | Active | cRGD | 91 |
| Enzyme responsive size-changeable gold NPs | Cediranib | Enhanced tumor vascular permeability, significant therapeutic effect | Passive | - | 168 |
| Poly(lactic-co-glycolic acid) (PLGA)-PEG NPs | Cediranib Verteporfin |
Combination drug therapy with phototherapy resulted in significant in vitro cytotoxicity. | Passive | - | 169 |
| Poly(styrene-co-maleic acid) micelles | Crizotinib Dasatinib |
Enhanced drug activity of drugs in combination, same anti-proliferative effect in vitro as free drug, potent anti-proliferative effect in vivo. | Passive | - | 170 |
| Human serum albumin (HSA) NPs | Dasatinib | As effective as free drug, reduced endothelial hyperpermeability | Passive | - | 171 |
| Poly-L-lactic acid(PLA) NPs modified with polyethyleneimine | Dasatinib Trastuzumab |
Better in vitro efficacy and sustained release of dasatinib | Active | Anti-HER2 antibody | 172 |
| Poly(Cyclohexene Phthalate) NPs | Dasatinib | Superior in vitro efficacy | Passive | - | 173 |
| PLGA NPs | Dasatinib | Compared to free drug enhanced inhibition of proliferative vitreoretinopathy related cellular contraction. | Passive | - | 174 |
| PLGA-conjugated gold NPs | Dasatinib | Enhanced growth inhibition in vitro and bioavailability in vivo | Passive | - | 175 |
| Magnetic micelles | Dasatinib | Increased in vitro cytotoxicity and decreased cellular migration | Active | Lactoferrin | 176 |
| CdSe/ZnS quantum dots | Desmethyl Erlotinib | Cytotoxic enhancement | Passive | - | 177 |
| Nanoparticular platform utilizing fat and supercritical fluid | Erlotinib | Improved water solubility | Passive | - | 178 |
| Magnetic iron oxide NPs | Erlotinib | Enhancement of therapeutic efficacy, MRI visualization | Passive | - | 142 |
| Nanocrystals formulation | Erlotinib | Solubility and drug efficacy enhancement | Passive | - | 179 |
| Folate-conjugated thermosensitive O‑maleoyl modified chitosan micellar NPs | Erlotinib | Significantly enhanced cytotoxicity | Active | Folate | 180 |
| Solid lipid NPs | Erlotinib | Higher anticancer activity than free drug | Passive | - | 181 |
| Nanoparticulation platform utilizing fat and supercritical fluid | Erlotinib | More potent in inhibiting EGF signaling and in suppressing tumor cell proliferation. | Passive | - | 182 |
| Cyclodextrin nanosponge | Erlotinib | Increase of solubility, dissolution and oral bioavailability, higher cellular uptake and in vitro cytotoxicity. | Passive | - | 183 |
| Polyamidoamine dendrimers | Erlotinib Survivin shRNA Chloroquine |
Promoted drug delivery and enhanced drug efficacy | Active | Anti-EGFR aptamer | 114 |
| Anti-EGFR aptamer-modified liposomal complexes | Erlotinib O2 |
Superior anti-tumor activity, significant inhibition of cell proliferation and improved apoptosis induction. | Active | Anti-EGFR aptamer | 105 |
| Eudragit® RL100 | Gefitinib | Enhanced oral bioavailability | Passive | - | 184 |
| Human heavy chain apoferritin | Gefitinib | Enhanced anti-tumor activity against HER2 overexpressing SKBR3 breast cancer cell line; decreased uptake in cell line, which does not express HER2. | Passive | - | 185 |
| Gold colloidal NPs | Gefitinib | Greater cytotoxicity | Passive | - | 186 |
| Gelatin tri-block NPs | Gefitinib Cetuximab siRNA |
Effective targeting and high bioavailability, very specific for KRAS G12C | Active | Anti-EGFR antibody | 117 |
| PEG-PLA NPs | Gefitinib Cyclosporin A |
Improvement of drug efficacy, sensitization of gefitinib resistant cells | Passive | - | 187 |
| Chitosan NPs | Gefitinib Chloroquine | Potential to overcome acquired resistance and improve cancer treatment efficacy. | Passive | - | 106 |
| Anti‐PD‐L1‐modified liposomal system | Gefitinib Simvastatin |
Remodeling the tumor microenvironment, reversing gefitinib resistance and enhancing EGFR T790M‐mutated NSCLC treatment outcomes. | Active | Anti-PD-L1 nanobody | 121 |
| Sialic acid-stearic acid conjugate modified on the surface of nanocomplexes | Ibrutinib | Suppressed tumor progression | Active | Sialic acid | 188 |
| HSA NPs | Imatinib base | 35% greater cytotoxicity | Passive | - | 189 |
| Galactoxyloglucan NPs | Imatinib mesylate | Enhancement of cytotoxic potential and reversal of multidrug resistance | Passive | - | 190 |
| PLGA NPs | Imatinib mesylate | Improved cytotoxic compared to free drug, 28 day‑long oral administration showed no significant cardiotoxicity or associated changes. | Passive | - | 87 |
| Poly(ε-caprolactone) NPs with chitosan | Imatinib mesylate | Improved drug's kinetics and efficacy, long-lasting inactivation of BCR-ABL autokinase activity. | Passive | - | 191 |
| Polycaprolactone nanocapsules | Lapatinib | Improvement of anti-tumor effects | Passive | - | 192 |
| Hyaluronic acid-D-α-tocopherol succinate-(4-carboxybutyl)triphenyl phosphonium bromide-based NPs (HA-TS-TPP) | Lapatinib | Better tumor growth suppression, triple negative breast cancer targeting | Active | HA; TS; TPP | 193 |
| HSA NPs | Lapatinib | Enhanced cell cytotoxicity and induction of apoptosis, inhibition of HER2 phosphorylation and superior anti-tumor efficacy in vivo, no subchronic toxicity within 60 days of treatment. | Passive | - | 88 |
| HSA NPs | Lapatinib | Inhibition of adhesion, migration and invasion ability of cells more effectively; extension of median survival time in mice. | Passive | - | 89 |
| HSA NPs | Lapatinib | Increased accumulation of Lapatinib in tumor tissue, better suppression effects both on primary breast cancer and lung metastasis in vivo. | Passive | - | 194 |
| PTX NPs and LAPA microparticles in a thermosensitive hydrogel | Lapatinib Paclitaxel |
Synergistic effect of LAPA and PTX on cell line overexpressing HER2 and P-gp; significantly less nonspecific toxicity. | Passive | - | 115 |
| Liposomes | Ponatinib | Significant tumor growth inhibition (by 60.4%) and markedly reduced side effects. | Passive | - | 195 |
| Liposomes | Nintedanib | Significant tumor growth inhibition (by 60.4%) and markedly reduced side effects. | Passive | - | 195 |
| Linear-dendritic self-assembling polymeric drug carrier release-triggered by enzyme Cathepsin B | Saracatinib | Better suppression of metastasis | Passive | - | 196 |
| Reduced graphene oxide nanosheets | Sorafenib | Improved cytotoxicity | Passive | - | 197 |
| Lipid nanocapsules | Sorafenib | Early tumor vascular normalization, decreased proliferation | Passive | - | 198 |
| Focused ultrasound-triggered thermosensitive liposomes | Sorafenib | Significantly lower cell viability | Passive | - | 90 |
| Self-assembling PEG-vitamin E succinate derivative NPs | Sorafenib Curcumin |
Enhanced in vitro cytotoxicity and anti-angiogenesis, greater drug concentration in organs in vivo and inhibition of tumor growth. | Passive | - | 132 |
| HSA encapsulated gold nanorods paired with photothermal ablation | Sorafenib | 100% tumor cell kill rate | Passive | - | 199 |
| Irradiated HSA gold nanorods | Sorafenib | Significantly induced hyperthermia, enhanced cytotoxicity | Passive | - | 200 |
| PLA-PEG-poly(L)-lysine-diethylenetriamine pentaacetic acid NPs with gadolinium and poly(L-histidine)-PEG-biotin modification | Sorafenib | Improved diagnostic abilities, higher anti-tumor effect in vitro and in vivo. | Active | Anti-VEGFR antibody | 141 |
| Styrene-co-maleic acid micelles | Sorafenib Nilotinib |
Greater cytotoxicity, decreased cell proliferation, increased apoptosis relative to the free TKIs. | Passive | - | 110 |
| Lactobionic acid modified and pH-sensitive chitosan-conjugated mesoporous silica nanocomplex | Sorafenib Ursolic acid |
Enhanced bioavailability, synergistic cytotoxicity, significant increase of cellular apoptosis and down-regulation of EGFR and VEGFR2 proteins expression, significant reduction of tumor burden in hepatocellular carcinoma. | Active | Lactobionic acid | 122 |
| Integrin-targeted cAmpRGD liposomes | Sunitinib | Inhibition of growth and adhesion, anti-angiogenic effect | Active | cAmpRGD | 201 |
| Self-nanoemulsifying drug delivery system | Sunitinib | Bioavailability and cytotoxicity increase | Passive | - | 79 |
| PLGA-PEG-MBA polymeric micelles combined with mannose-modified lipid calcium phosphate NPs-based Trp2 vaccine | Sunitinib | Abrogation of tumor-associated immune suppression, enhanced therapeutic efficacy. | Passive | - | 119 |
| Self-nanoemulsifying drug delivery system | Sunitinib malate | Two-fold increase in efficacy | Passive | - | 202 |
| PEG-NLG919-based immunostimulatory nanocarrier | Sunitinib Paclitaxel NLG919 |
More active tumor immune microenvironment and further improved anti-tumor activity. | Passive | - | 203 |
| BSA-coated superparamagnetic iron oxide NPs | Sunitinib Curcumin |
Significant tumor inhibition yet least drug-induced toxicity both in vitro and in vivo when compared with free drug formulations. | Passive | - | 104 |
| iRGD-PEG-PLA NPs | Vandetanib | More effective cytotoxic activity in vitro and tumor inhibition in vivo | Active | iRGD | 204 |
| Micellar gold NPs | Vandetanib | Inhibition of tumor growth | Passive | - | 205 |