Table 3.
Characteristics of nanotechnology based flavonoids as anticancer agents
| Flavonoids | Material & Technology | Size (nm) | Target | Dose | Activity | References |
|---|---|---|---|---|---|---|
| Genistein | GenLip HSPC main | < 407 | Murine breast cancer (4T1), human ovarian cancer(OVCAR-3), prostate cancer(PC-3) | 22.7–34.1 µM (IC50) | DNA laddering and apoptosis with 1/3 concentration of free G | Phan et al., (2013) |
| Quercetin | PMAA-NP | – | Cervix cancer (HeLa) | 100 µM | 87% reduction of viability vs free Q, and 95% suppression of viability vs control | |
| CNT-PMAA-NP | 80 | Cervix cancer (HeLa) | 10 µM (IC50) | Inhibit cell proliferation and DNA condensation strongerly | ||
| LsbPMS | 92.2 | Breast cancer (MCF-7) | 1.4 µM (IC50) | Inhibit cell proliferation vs free Q (IC50: > 30 µM) | ||
| Breast cancer (SKBR-3) | 4.63 µM (IC50) | Inhibit cell proliferation vs free Q (IC50: > 30 µM) | ||||
| CT-26 Xenograft mice |
50 mg/Kg, i.v. 7 days |
No significant reduction of tumor volume vs free Q |
Pouci et al., (2012) Cirillo et al., (2013) Chang et al., (2018) |
|||
| EGCG | PLA-PEG-NP | 260 |
Prostate cancer (PC-3) PC-3 xenograft mice |
3.74 µM (IC50) 100 µg/mice/d i.p., thrice/wk, 3 wks |
Inhibit cell proliferation and prolong half life Reduction of tumor volume almost same as free EGCG(1 mg/mice/d)group |
Siddigui et al., (2009) |
|
PNG-EGCG Chitosan-NP |
– 180 |
Bladder cancer (MBT-2) MBT-2 xenograft mice Melanoma(Mel 928) Mel 928 xenograft mice |
4.3 ppm (IC50) 2 mg EGCG + 1.5 ppm PNG/mice 7 µM (IC50) 100 µg/mice i.g. 5 times/wk, 3 wks |
Inhibit cell proliferation vs free E (IC50:28.4 µM) 70% reduction of tumor volume vs free E (2 mg) Inhibit cell proliferation vs free E (IC50:53 µM) 28% reduction of tumor volume vs free E (1 mg/mice), PSA↓ |
Heish et al., (2011) Siddigui et al., (2014) |
|
| CSLIPO | 85 | Breast cancer(MCF-7) |
10 µM (IC40) 100 µM |
50% reduction of viability vs free E Increase cellular E contents 34 times vs free E |
de Pace et al., (2013) | |
| Chit-NP | 200 < | PCa xenograft mice | 6 mg/Kg i.g. 3 wks | 50% reduction of tumor volume vs free E (40 mg/Kg) | Khan et al., (2014) | |
| PLGA-PEG-NP | 251 |
Prostate cancer (LNCaP, PC-3, DU-145) 22 Rv 1 xenograft mice |
20 µM 100 µg/mice/d i.v 5 times/wk, 3 wks |
40% reduction of viability vs free E 40% reduction of tumor volume vs free E (1 mg/mice/d) |
Sanna et al., (2017) | |
| Luteolin | PLA-PEG-OMe-NP | 115 |
Head and neck cancer (Tu212) Tu212 xenograft mice |
4.13 µM (IC50) 3.3 mg/Kg i.p. every 2 days, 30 days |
Slight reduction of viability vs free L (IC50:6.96 µM) 25% reduction of tumor volume vs free L |
Majumdar et al., (2014) |
| Lipo-Lut | 105 | Prostate cancer (CT-26) |
20 µM (IC50) 50 mg/Kg, i.v. 5 times, every 2 days |
Inhibit cell proliferation vs free L (IC50: > 60 µM) 70% reduction of tumor volume vs free L, Inhibit tumor vascularization, prolong plasma concentration |
Wu et al., (2018a) | |
| Hesperetin | CFH-NP | 450 | Colon cancer (HCT-15) | 28 µM (IC50) | Inhibit cell proliferation vs free H (IC50:190 µM) and inhibit apoptotic gene | Lazer et al., (2018) |
The undescribed amounts of doses of free G, free Q, free E and free L are the same with the amounts of doses of genistein-NP, quercetin-NP, EGCG-NP and luteolin-NP, respectively. Some reduction percentages are adjusted from the original data. Lip or Lipo: liposome, HSPC: fully-hydrogenated soy phosphatidylcholine, NP: nanopanticle, PMAA: polymetha acrylic acid, CNT: carbon nanotube, LsbPMS: lecithin-stabilized polymeric micelles, PNG: nanogold particle, PSA: prostate cancer specific antigen, CSLIPO: chitosan-coated nanoliposome, Chit: chitosan, PLGA-PEG: poly-(lactide-co-glyco syl)-carboxylic acid- polyethyleneglycol, PLA-PEG: polylactic acid-polyethyleneglycol, OMe: methanol, CFH: chitosan folate hesperetin, EGCG: epigallocatechin-3-gallate, Q: quercetin, L: luteolin, G: genistein, H: hesperetin, d:day, wk: week