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. 2018 Dec 16;10(4):282. doi: 10.3390/pharmaceutics10040282

Table 3.

Therapeutic outcomes and toxicity evaluation of graphene-based nanomaterials containing GO, NGO, rGO and GQDs.

Graphene-Based Nanomaterial (GBNs) In Vitro In Vivo Ref
Cell Model Dark Cell Viability [GBNs]
(Method)		 NIR Laser Drug or Active, Dose,
AL(wt%)		 Therapeutic Outcomes
[GBNs]
(Method)		 Animal Model
and Dose		 Toxicity
(Method)		 NIR Laser Drug or Active, Dose,
AL(wt%)		 Therapeutic Outcomes
(Method)
Therapeutic outcomes and toxicity evaluation of graphene-based nanomaterials containing GO
Au@PLA-(PAH/GO)n HeLa
HUVECs		 90% HUVECs viability with
1000 µg/mL
(Trypan blue)		 λ = 808 nm
P = 6.67 W/cm2
t = 6 min		 ―

  • ΔT = 21 °C

  • 0.1 < IC50 < 0.25 µg/mL

  • >80% HeLa cell death with 0.5 µg/mL

    (Trypan blue)

 Xenograft mice (HT1080 cells)
20 mg/Kg

  • Minimal effects

    (body weight)

 λ = 808 nm
P = 2.23 W/cm2
t = 10 min		 ―

  • ΔT = 18.6 °C

  • Tumor reduced ≈80% in 5d (volume)

 [61]
UCNPs-NGO/ZnPc KB
HeLa		 >90% with
320 µg/mL
(MTT)		 - PDT:
λ = 630 nm
P = 50 mW/cm2
t = n.r.
- PTT:
λ = 808 nm
P = 2 W/cm2
t = 10 min		 ZnPc
n.r.

  • ΔT = 23 °C

  • 40 < IC50 < 80 µg/mL

  • 90% cell death with 320 µg/mL

    (MTT)

 ― ― ― ― ― [85]
GO-HA-Ce6 A549 ≈84% with
1.8 µM Ce6
(CCK-8)		 λ = 810 nm
P = 4 W/cm2
t = 8 min		 ―

  • ΔT = 27 °C

  • IC50 n.r.

  • 90% cell death with 1.8 µM Ce6

    (CCK-8)

 ― ― ― ― ― [52]
ICG-GO-FA HeLa ≈100% with
20 µg/mL
(MTT)		 λ = 808 nm
P = 2 W/cm2
t = 10 min		 ―

  • ΔT ≈ 40 °C

  • IC50 n.r.

  • >90% cell death with 20 µg/mL

    (MTT)

 ― ― ― ― ― [86]
GO-AuNS SKBR-3
MCF-10a		 ≈95% in
SKBR-3 and MCF-10a with 40 µg/mL
(MTT)		 λ = 808
P = 0.75 W/cm2
t = 2		 ―

  • ΔT = 60 °C

  • IC50 n.r.

  • 81% cell death with 10 µg/mL

    (MTT)

 ― ― ― ― ― [70]
GQD-Cur HCT166 >90% with
100 µg/mL
(SRB)		 ― Cur
AL ≈ 41%

  • ΔT = 18 °C

  • 6 < IC50 < 12.5 µg/mL

  • >90% cell death with 100 µg/mL

    (SRB)

 Xenograft mice (HCT166)
10 mg/Kg

  • Minimal effects

    (body weight)

  • Undetectable tissue damage (histological)

 ― Cur
AL ≈ 41%

  • Tumor growth reduced 4× in

    14 d

    (volume)

 [78]
GO-Abs/Cy7 U87-MG ≈95% with
42.8 µg/mL
(CCK-8)		 λ = n.r.
P = 0.016W/cm2
t = n.r.		 ―

  • 5.3 < IC50 < 10.7 µg/mL

  • >90% cell death with 16.05 µg/mL

    (CCK-8)

 Xenograft mice (U87-MG cells)
43.4 µg/mouse

  • Minimal effects

    (body weight)

  • Minimal tissue damage

    (histological)

 λ = 753 nm
P = 0.02 W/cm2
t = 1 min		 ―

  • Tumor did not grow in 20 d and was 7× smaller than control

  • Survival ≥ 20 d

  • Noticeable tumor tissue damage

    (histological)

 [72]
GDH MDCK
A549		 ≈80–85% MDCK cell viability
with 100 µg/mL
(MTT)		 λ = 670 nm
P = 1 W/cm2
t = 5 min		 DOX
100 μg/mL
AL n.r.

  • ΔT ≈ 30 °C

  • IC50 = 50 µg/mL

  • 70–75% A549 cell death with 100 µg/mL

    (MTT)

 Xenograft mice (A549 cells)
2.5 mg/Kg

  • Minimal effects

    (body weight)

  • Minimal tissue damage

    (histological)

 λ = 670 nm
P = 1 W/cm2
t = 30 min		 DOX
n.r.

  • ΔT ≈ 17 °C

  • Tumor reduced ≈40% in 18 d (volume)

  • Noticeable tumor tissue damage

  • (histological)

 [62]
PheoA+GO:FA-BSA-c-PheoA B16F10
MCF-7		 100% with
0.375 µg/mL
(MTT)		 λ = 670 nm
P = 0.13 W/cm2
t = 10 min		 ―

  • ΔT = 6 °C

  • IC50 < 0.375 µg/mL

  • 95% cell death with 1.5 µg/mL

    (MTT)

 Xenograft mice (B16F10 cells)
2 mg/Kg

  • Minimal effects

    (body weight)

 λ = 670 nm
P = 0.13 W/cm2
t = 10 min		 ―

  • Tumor growth reduced 3× in 14 d (volume)

 [47]
GO-PEG-ZnS:Mn-DOX HeLa;
CHO-K1		 100% with 1000 µg/mL
(w/o DOX)
(MTT)		 ― DOX
300 μg/mL
AL ≈ 10%

  • IC50 < 2.5 µg/mL

  • 85% cell death with 10 µg/mL

    (MTT)

 ― ― ― ― ― [53]
CPGA SCC7 ≈70% with
200 µg/mL
(MTT)		 λ = 808 nm
P = 0.3 W/cm2
t = 10 min		 ―

  • ΔT = 23 °C

  • 50 < IC50 <100 µg/mL

  • 80% cell death with 200 µg/mL

    (MTT)

 Xenograft mice (SCC7 cells)
10 mg/Kg

  • Minimal effects

    (body weight)

 λ = 808 nm
P = 0.75 W/cm2
t = 10 min		 ―

  • ΔT = 15.9 °C

  • Tumor abl.

    in 6 d

    (volume)

 [56]
GO@Gd-PEG-FA/DOX MCF-7 ≈85% with
10 µg/mL
(w/o DOX)
(SRB)		 λ = 808 nm
P = 2.5 W/cm2
t = 5 min		 DOX
10 µg/mL
AL≈94%

  • ΔT = 22.1 °C

  • IC50 n.r.

  • 80% cell death with 10 µg/mL

    (SRB)

 Xenograft mice (S180 cells)
10 mg/Kg

  • Minimal effects

    (body weight)

 λ = 808 nm
P = 2 W/cm2
t = 5 min		 DOX
5 mg/kg
AL ≈ 94%

  • ΔT = 9.6 °C

  • Tumor growth reduced 7× in 12 d (volume)

  • Noticeable tumor tissue damage

    (histological)

 [75]
GO/AuNS-
-PEG/Ce6		 EMT6 >95% with
100 µg/mL (CCK-8)		 λ = 660 nm
P = 2 W/cm2
t = 8 min		 ―

  • ΔT = 50 °C

  • IC50 < 0.375 µg/mL

  • ≈80% cell death with 150 µg/mL

    (CCK-8)

 Xenograft mice (EMT6 cells)
10 mg/kg

  • Minimal effects

    (body weight)

  • Minimal tissue damage

    (histological)

 λ = 660 nm
P = 3 W/cm2
t = 10 min		 ―

  • ΔT = 20 °C

  • Tumor abl.

    in 14 d (volume)

  • Noticeable tumor tissue damage

    (histological)

 [87]
GO/Bi2Se3/
PVP		 HeLa >90% with
75 µg/mL (MTT)		 λ = 808 nm
P = 0.3 W/cm2
t = 10 min		 ―

  • ΔT = 33 °C

  • 25 < IC50 < 50 µg/mL

  • ≈90% cell death with 100 µg/mL (MTT)

 Xenograft mice (HeLa)
0.2 mg/mouse

  • Minimal effects

    (body weight)

  • Minimal tissue damage with 0.4 mg/mouse

    (histological)

 λ = 808 nm
P = 0.4 W/cm2
t = 5 min		 ―

  • ΔT = 23 °C

  • Tumor abl.

    in 2 d (volume)

  • Noticeable tumor tissue damage

    (histological)

 [92]
GO/UCNPs ZnFe2O4 HeLa;
L929		 80% with
500 µg/mL (MTT)		 λ = 980 nm
P = 0.8 W/cm2
t = 15 min		 ―

  • ΔT ≈ 55 °C

  • IC50 < 15.6 µg/mL

  • ≈90% cell death with 500 µg/mL

    (MTT)

 Xenograft mice (U14 cells)
n.r.

  • Minimal effects

    (body weight)

  • Minimal tissue damage

    (histological)

 λ = 980 nm
P = 0.8 W/cm2
t = 15 min		 ―

  • ΔT ≈ 35 °C

  • Tumor did not grow in 14 d and was 7× smaller than control (volume)

  • Noticeable tumor tissue damage

    (histological)

 [48]
GO/MnWO4/PEG 4T1
HUVEC		 90% and 80% (4T1 and HUVEC cell) with 100 µg/mL
(MTT)		 λ = 808 nm
P = 0.6 W/cm2
t = 10 min		 DOX
5 µg/mL
AL ≈ 55%

  • ΔT ≈ 55 °C

  • IC50 < 50 µg/mL

  • ≈90% cell death with 100 µg/mL

    (MTT)

 Xenograft mice (U14 cells)
0.6 mg/mouse

  • Minimal effects

    (body weight)

  • Minimal tissue damage

    (histological)

 λ = 808 nm
P = 0.6 W/cm2
t = 10 min		 DOX
0.2 mg/mouse
AL ≈ 55%

  • ΔT ≈ 27 °C

  • Tumor abl.

    in 12 d.

    (volume)

  • Noticeable tumor tissue damage

    (histological)

 [5]
LOGr-Pc-LHRH A2780/AD
RBC

  • 90% (A2780/AD) with 125 µg/mL

    (MTT)

  • Minimal hemolytic activity (RBC) with 44 µg/mL

 λ = 690 nm
P = 0.95W/cm2
t = 15 min		 Pc
4 µg/mL

  • ΔT ≈ 35 °C

  • IC50 < 1.8 µg/mL

  • ≈95% cell death with 7 µg/mL

    (Calcein AM)

 Xenograft mice (A2780/AD
cells)
1 mg/Kg		 ― ― ―

  • Only diagnostic

    by fluorescence tumor imaging

 [81]
Therapeutic outcomes and toxicity evaluation of graphene-based nanomaterials containing NGO
GO-DOX ― ― ― ― ― Xenograft mice (H1975 cells)
n.r.

  • Undetectable tissue damage (histological)

  • Minimal effects (body weight)

 ― DOX
8 mg/kg
AL = 133%

  • Tumor reduced ≈75% in 14 d (volume)

 [71]
ICG-FeCl3@GO G361 ― λ = 785 nm
P = 1 W/cm2
t = 20 min		 ICG
n.r.

  • IC50 n.r.

  • 99% cell death [GBNs] n.r

    (MTT, Trypan blue)

 ― ― ― ― ― [83]
GO@Ag-DOX-NGR MCF-7 ≈90% with
10 µg/mL
(SRB)		 λ = 808 nm
P = 2 W/cm2
t = 3 min		 DOX
4 µg/mL
AL ≈ 82%

  • ΔT = 18 °C

  • 0.5 < IC50 < 1 µg/mL

  • ≈94% cell death with 4.88 µg/mL

    (SRB)

 Xenograft mice (S180)
6.1 mg/Kg

  • Minimal effects

    (body weight)

  • Minimal tissue damage

    (histological)

 λ = 808 nm
P = 2 W/cm2
t = 3 min		 DOX
5 mg/kg
AL ≈ 82%

  • Tumor did not grow in 13 d and was 5× smaller than control

  • Survival≥ 14 d

  • Noticeable tumor tissue damage

    (histological)

 [76]
GO-PEG-DVDMS PC9 ≈70% with
3 µg/mL
(MTT)		 - PDT:
λ = 630 nm
P = 3 J/well
t = n.r.

- PTT:
λ = 808 nm
P = 1 W/cm2
t = 3 min		 DVDMS
n.r

  • IC50 ≈ 0.25 µg/mL

  • 90% cell death with 3 µg/mL

    (MTT)

 Xenograft mice (PC9 cells)
1 mg/Kg

  • Minimal effects

    (body weight)

 - PDT:
λ = 630 nm
50 J
t = n.r.

- PTT:
λ = 808 nm
P = 1 W/cm2
t = 10 min		 DVDMS
2 mg/kg

  • ΔT = 25 °C

  • Tumor abl.

    in 2 d

    (volume)

 [88]
IO/GO-COOH HeLa 95% with
[Fe] = 200 µg/mL
(MTT)		 λ = 808 nm
P = 2 W/cm2
t = 5 min		 ―

  • ΔT = 60 °C

  • IC50 n.r.

  • ≈100% cell death with 150 µg/mL

    (MTT)

 Xenograft mice (S180 cells)
37.5 µg /mouse

  • Minimal effects

    (body weight)

 λ = 808 nm
P = 1 W/cm2
t = 5 min		 ―

  • ΔT > 37 °C

  • Tumor abl.

    in 2 d (volume)

  • Survival ≥ 60 d

 [60]
GO-PEG-CysCOOH 4T1 ≈100% with
250 µg/mL (MTT)		 λ = 808 nm
P = 0.5 W/cm2
t = 3 min		 ―

  • ΔT ≈ 25 °C

  • IC50 n.r.

  • >90% cell death with 250 µg/mL

    (MTT)

 Xenograft mice (4T1)
450 μg/mouse

  • No detectable effects

    (body weight)

  • Minimal tissue damage

    (histological)

 λ = 808 nm
P = 0.5 W/cm2
t = 5 min		 ―

  • ΔT ≈ 38 °C

  • Tumor abl.

    in 2 d(volume)

  • Survival ≥ 60 d

 [73]
Au@NGO HeLa cells ≈80% with
200 µg/mL
(MTT)		 ― DOX
25 µg/mL
AL ≈ 2%

  • 0.375 < IC50 = 1.25 µg/mL

  • >90% cell death with 2 µg/mL

    (MTT)

 ― ― ― ― ― [68]
NGO-PEG-FA B16F0 ≈90% with
75 µg/mL
(MTT)

  • PTT


λ = 808 nm
P = 0.32 W/cm2
t = 15 min

  • PTT+PDT


λ = 980 nm
P = 0.32 W/cm2
t = 18 min		 ―
  • -
    PTT
    • ΔT ≈ 18 °C
    • 50 < IC50 < 75 µg/mL
    • 65% cell death with 75 µg/mL

  • -
    PTT+PDT:
    • ΔT ≈ 11 °C
    • IC50 = 25 µg/mL
    • 85% cell death with 75 µg/mL
      (MTT)
 Xenograft mice (B16F10 cells)
8 mg/Kg		 ―

  • PTT


λ = 808 n
P = 0.25 W/cm
t = 8 mi

  • PTT+PDT


λ = 980 nm
P = 0.25 W/cm2
t = 10 min		 ―
  • -
    PTT:
    • ΔT = 8.8 °C
    • Tumor slow growth in 14 d
    • Survival ≤ 32 d

  • -
    PDT+PTT:
    • ΔT = 1.8 °C
    • Tumor abl. in 14 d (volume)
      Survival ≥ 40 d
 [7]
NGO-IR-808 A549;
Lewis lung		 Negligible toxicity with
10 µM
(CCK-8)		 λ = 808 nm
P = 2 W/cm2
t = 5 min		 ―

  • ΔT = 34 °C

  • -
    A549 cells:
    • IC50 = 5 µg/mL
    • 95% cell death with 10 µM
  • -
    Lewis lung cells:
    • 2.5 < IC50 <5 µg/mL
    • 100% cell death with 10 µM
      (CCK-8)
 Xenograft mice (A549; Lewis lung cells)
10 mg/Kg

  • No detectable effects

    (body weight)

  • Minimal tissue damage

    (histological)

 λ = 808 nm
P = 1 W/cm2
t = 5 min		 ―

  • ΔT = 23.5 °C

  • Tumor abl.

    in 3–4 d.

    (volume)

  • Noticeable tumor tissue damage

    (histological)

 [67]
NGO-PEG-ICG/PTX MG-63 ≈100% with
200 µg/mL
(w/o PTX)
(CCK-8)		 ― PTX
100 µg/mL
AL ≈ 90%

  • IC50 = 20 µg/mL

  • 90% cell death with 100 µg/mL of PTX

    (CCK-8)

 Xenograft mice (MG-63)
10 mg/kg

  • No detectable effects

    (body weight)

  • Minimal tissue damage

    (histological)

 ― PTX
9 mg/kg
AL ≈ 90%

  • Tumor abl.

    in 15 d

    (volume)

  • Noticeable tumor tissue damage

    (histological)

 [91]
NGO-UCNPs-Ce6 HeLa;
L929		 >95% with
800 µg/mL
(MTT)		 λ = 808 nm
P = 0.72 W/cm2
t = 10 min		 ―

  • ΔT = 47 °C

  • IC50 = 25 µg/mL

  • 85% cell death with 800 µg/mL (MTT)

 Xenograft mice (U14 cells)
n.r.

  • No detectable effects

    (body weight)

  • Minimal tissue damage

    (histological)

 λ = 808 nm
P = 0.72 W/cm2
t = 10 min		 ―

  • Tumor did not grow in 14 d and was 9× smaller than control

    (volume)

  • Noticeable tumor tissue damage

    (histological)

 [57]
UCNP@
NGO		 4T1 >90% with
400 µg/mL
(MTT)		 λ = 808 nm
P = 2 W/cm2
t = 10 min		 ―

  • ΔT = 47 °C

  • IC50 = 100 µg/mL

  • >90% cell death with 400 µg/mL (MTT, Cytometry)

 Xenograft mice (4T1 cells)
n.r.

  • Minimal effects

    (body weight)

  • Minimal tissue damage

    (histological)

 λ = 808 nm
P = 1 W/cm2
t = 5 min		 ―

  • ΔT = 23 °C

  • Tumor abl.

    in 6 d

    (volume)

 [64]
Therapeutic outcomes and toxicity evaluation of graphene-based nanomaterials containing rGO
BSA/nano-rGO MCF-7 cells 100% with
0.04 µg/mL
(MTT)		 λ = 808 nm
P = 6 W/cm2
t = 5 min		 ―

  • ΔT = 30 °C

  • IC50 = 0.108 µg/mL

  • 80% cell death with 0.15 µg/mL

    (MTT)

 Xenograft mice (MCF-7)
20 mg/kg

  • Undetectable tissue damage (histological)

 λ = 808 nm
P = 0.6 W/cm2
t = 5 min		 ―

  • ΔT = 18 °C

  • Noticeable tumor tissue damage

    (histological)

 [74]
rGONM-PEG-Cy7-RGD ― ― ― ― ― Xenograft mice (U87MG cells)
0.2 mg/mouse

  • Minimal effects

    (body weight)

 λ = 808 nm
P = 0.1 W/cm2
t = 7 min		 ―

  • Tumor abl.

    in 3 d

    (volume)

  • Survival ≥ 90 d

 [46]
rGO-
Fe2O3@Au
NPs		 HeLa ≈90% with
50 µg/mL
(MTT)		 λ = 808 nm
P = 2 W/cm2
t = 5 min		 DOX
n.r.
AL≈100%

  • ΔT = 30 °C

  • 10 < IC50 < 20 µg/mL

  • 97% cell death with 50 µg/mL (MTT)

 ― ― ― ― ― [50]
rGO nanosheets KB ≈95% with
20 µg/mL
(CCK-8)		 λ = 808 nm
P = 1.2 W/cm2
t = 3 min		 ―

  • ΔT = 51 °C

  • IC50 n.r.

  • >90% cell death with 20 µg/mL

    (CCK-8)

 Xenograft and orthotopic mice (KB cells)
5 mg/kg

  • Minimal effects

    (body weight)

 λ = 808 nm
P = 1.2 W/cm2
t = 3 min		 ―

  • ΔT = 13 °C

    Tumor abl.

    in 3 d

    (volume)

  • highest % of apoptotic cells

    (histological)

  • Survival ≥ 50 d

 [69]
131I-RGO-PEG 4T1 ≈90% with
200 µg/mL
(CCK-8)		 λ = 808 nm
P = 0.5 W/cm2
t = 10 min		 131I
100 µCi

  • ΔT = 51 °C

  • IC50 n.r.

  • 90% cell death with 100 µg/mL

    (CCK-8)

 Xenograft and orthotopic mice (4T1cells)
10 mg/kg

  • Minimal effects

    (body weight)

 λ = 808 nm
P = 0.2 W/cm2
T = 20 min		 131I
200 µCi/ mouse

  • ΔT ≈ 18 °C

  • Tumor abl.

    in 16 d

    (volume)

  • Noticeable tumor tissue damage

    (histological)

 [51]
rGO-AuNRVe U87MG 100%
with 2.4 nM
(CCK-8)		 λ = 808 nm
P = 0.25 W/cm2
t = 5 min		 DOX
6.4 µg/mL
AL ≈ 65%

  • IC50 = 0.63 µg/mL (DOX)

  • 90% cell death with 6.4 µg/mL of DOX

    (CCK-8)

 Xenograft and orthotopic mice (U87MG)
10 mg/kg

  • Minimal effects

    (body weight)

  • Minimal tissue damage

    (histological)

 λ = 808 nm
P = 0.25 W/cm2
t = 5 min		 DOX
AL ≈ 65%

  • ΔT = 13 °C

  • Tumor abl.

    in 14 d

    (volume)

  • Survival≥ 40 d

 [79]
anti-EGFR-PEG-rGO@
CPSS-Au-R6G		 A549 100% with
100 µg/mL
(MTT)		 λ = 808 nm
P = 0.5 W/cm2
t = 5 min		 ―

  • IC50 n.r.

  • 72% cell death with 100 µg/mL

    (MTT)

 ― ― ― ― ― [6]
ICG-PDA-rGO 4T1 ≈90% with
20 µg/mL
(MTT)		 λ = 808 nm
P = 0.6 W/cm2
t = 5 min		 ―

  • ΔT = 30 °C

  • IC50 = 10 µg/mL

  • 85% cell death with 40 µg/mL

    (MTT)

 Xenograft and orthotopic mice (4T1 cells)
200 µg/mouse

  • Minimal effects

    (body weight)

 λ = 808 nm
P = 0.6 W/cm2
t = 5 min		 ―

  • Tumor abl.

    in 3 d

    (volume)

  • Survival ≥ 40 d

 [59]
rGO-GSPs U87MG ≈100% with
100 µg/mL
(MTT)		 λ = 808 nm
P = 0.8 W/cm2
t = 5 min		 ―

  • ΔT = 40 °C

  • IC50 n.r.

  • 85% cell death with 100 µg/mL

    (MTT)

 Xenograft mice (U87MG cells)
200 μg/mouse

  • No detectable tissue damage

    (histological)

 λ = 808 nm
P = 0.8 W/cm2
t = 5 min		 ―

  • ΔT = 28 °C

  • Tumor abl.

    in 2 d

    (volume)

  • Noticeable tumor tissue damage

    (histological)

  • Survival ≥ 40 d

 [66]
rGO-mfHSA HepG2 ≈100% with
20 μg/mL
(CCK-8)		 λ = 808 nm
P = 2 W/cm2
t = 5 min		 ―

  • ΔT ≈ 30 °C

  • IC50 = 10 μg/mL

  • >90% cell death

    (CCK-8)

 Xenograft mice (HepG2)
200 μg/mouse

  • No detectable effects

    (body weight)

 λ = 808 nm
P = 1 W/cm2
t = 10 min		 ―

  • ΔT ≈ 20 °C

  • Tumor growth. reduced 4× in 20 d (volume)

 [93]
FA-PEG-Lip@rGO/
Res		 A549
MCF-7		 >90% with
80 µg/mL
(w/o Res)
(MTT)		 λ = 780 nm
P = 0.6 W/cm2
t = 10 min		 Res
56 µg/mL
AL ≈ 70%

  • IC50 ≈ 10 µg/mL

  • >98% cell death with 80 µg/mL

    (MTT)

 Xenograft mice (MCF-7 cells)
2.2 mg/kg

  • No detectable effects

    (body weight)

 λ = 780 nm
P = 0.6 W/cm2
t = 5 min		 Res
AL ≈ 70%

  • ΔT = 17 °C

  • Tumor abl.

    in 10 d

    (volume)

 [58]
ArGO ― ― ― ― ― Xenograft mice (SCC7 cells)
5 mg/kg

  • 100% survival one day after i.v.;

  • normal blood test results

    (50 mg/kg)

 λ = 808 nm
P = 1.5 W/cm2
t = 3 min		 ―

  • ΔT = 16 °C

  • Tumor abl.

    in 10 d

    (volume)

  • Survival≥ 50 d

 [77]
AAP10-pDA/rGO MCF-7 ≈100% with
160 µg/mL
(MTT)		 λ = 808 nm
P = 1.5 W/cm2
t = 5 min		 AAP10
50 nM
AL ≈ 0.024%

  • ΔT = 18 °C

  • IC50 n.r.

  • ≈80% cell death with 120 µg/mL (MTT)

 Xenograft mice (4T1 cells)
0.3 mg/mouse

  • Minimal effects

    (body weight)

  • No detectable tissue damage

    (histological)

 λ = 808 nm
P = 1.5 W/cm2
t = 5 min		 AAP10
AL ≈ 0.024%

  • ΔT = 25 °C

  • Tumor abl.

    in 7 d

    (volume)

  • Noticeable tumor tissue damage

    (histological)

 [90]
Therapeutic outcomes and toxicity evaluation of graphene-based nanomaterials containing GQDs
cGdots MDA-MB231 >70% with
500 µg/mL
(MTT)		 λ = 670 nm
P = 0.3 W/cm2
t = 30 min		 ―

  • ΔT ≈ 25 °C

  • IC50 ≤ 50 µg/mL

  • >70% cell death with 500 µg/mL (MTT)

 Xenograft mice (MDA-MB231 cells)
75 µg/mouse

  • No detectable effects

    (body weight)

 λ = 670 nm
P = 0.3 W/cm2
t = 30 min
irr. every other day		 ―

  • ΔT = 17 °C

  • Tumor growth reduced 2× in 14 d (volume)

  • Noticeable tumor tissue damage

    (histological)

 [45]
GQDs HeLa >90% with
1.8 µM
(MTT)		 λ = 670 nm
P = 6.5 mW/cm2
t = 10 min		 PpIX
n.r.

  • 0.036 < IC50 < 0.09 µM

  • >80% cell death with 1.8 µM (MTT)

 Xenograft mice (MDA-MB231 cells)
80 µg/mouse

  • No detectable effects

    (body weight)

 λ = 400–800 nm
P = 80 mW/cm2
t = 10 min
irr. day 1 and 7		 PpIX
n.r.

  • Tumor abl.

    in 20 d

    (volume)

 [44]
PLA-PEG-grafted GQDs
(f-GQDs)		 HeLa ≈90% cell viability with 140 µg/mL
(MTT)		 ― IP and ASODN
50 nM

  • IC50 n.r.

  • 32% cell death with 14 µg/mL


(Cytometry)		 ― ― ― ― ― [55]
AS1411@
GQD		 A549 100% cell viability with 5 µM
(MTT)		 λ = 808 nm
P = 2 W/cm2
t = 10 min		 AS1411n.r.

  • ΔT ≈ 13 °C (in H2O)

  • 50% cell death with 5 µM

    (MTT)

 ― ― ― ― ― [84]
HA-GQD
-SiO2 NPs		 HeLa 100% with 4 µM Hypo-crellin
(MTT)		 λ = 470 nm Hypocre-llin
4 µM

  • IC50 n.r.

  • 80% cell death with 4 µM Hypocrellin

    (MTT)

 ― ― ― ― ― [94]
GQDs@Cys-BHC L929
HeLa
MDA-MB-231		 Low toxicity with
200 µg/mL (w/o BHC)
(Trypan blue, MTT)		 ― BHC
≈0.4 mM
AL ≈ 88%

  • IC50 = 200 µg/mL

  • 40–50% cell death with 200 µg/mL

    (Trypan blue, MTT)

 ― ― ― ― ― [82]
Fe3O4@SiO2
@GQDs-FA/DOX		 HeLa >90% with
50 µg/mL
(MTT)		 λ = 808 nm
P = 0.3 W/cm2
t = 10 min		 ―

  • IC50 = 1 µg/mL

  • 85% cell death with 50 µg/mL

    (MTT)

 ― ― ― ― ― [80]
GQD-MSN-
-DOX		 4T1 ≈95% with
100 μg/mL
(CCK-8)		 λ = 808 nm
P = 2.5 W/cm2
t = 3 min		 DOX
4.5 μg/mL
AL ≈ 4.8%

  • ΔT ≈ 20 °C

  • IC50 n.r.

  • ≈90% cell death with 100 µg/mL

    (CCK-8)

 ― ― ― ― ― [89]
GQD-PEG-P A549
MCF-7		 100% with
100 µg/mL
(MTT)		 λ = 980 + 636 nm
P = 0.72 W/cm2
t = 10 min		 ―

  • ΔT = 30 °C

  • IC50 n.r.

  • 90% cell death with 100 µg/mL

    (MTT)

 ― ― ― ― ― [49]
DOX@GQD-
-P-Cy		 4T1 ≈95% with
4 µg/mL
(w/o DOX)
(MTT)		 ― DOX
3.3 µg/mL
AL ≈ 82.5%

  • IC50 = 1 µg/mL

  • ≈98% cell death with 4 µg/mL

    (MTT)

 Xenograft mice (4T1 cells)
1 µg /mouse

  • Minimal effects

    (body weight)

 ― DOX
0.8 µg /mouse
AL ≈ 82.5%

  • Tumor growth decreased 4×

    (volume)

  • Noticeable tumor tissue damage

    (histological)

  • Survival ≤ 20 d

 [54]
DL-GQD-comp BT-474 ≈90% with
100 µg/mL
(w/o DOX)
(CCK-8)		 ― DOX
8.8 µM
AL ≈ 5.3%

  • 50 < IC50 < 100 µg/mL

  • ≈80% cell death with 100 µg/mL

    (CCK-8)

 ― ― ― ― ― [63]
IR780/GQD-FA HeLa ≈90% with
30 µg/mL
(CCK-8)		 λ = 808 nm
P = 1 W/cm2
t = 5 min		 ―

  • ΔT = 28 °C

  • IC50 = 10 µg/mL

  • ≈98% cell death with 30 µg/mL

    (CCK-8)

 Xenograft mice (HeLa cells)
2 mg/kg

  • No detectable effects

    (body weight)

 λ = 808 nm
P = 1 W/cm2
t = 5 min		 ―

  • ΔT = 23 °C

  • Tumor abl.

    in 6 d

    (volume)

  • Survival ≥ 60 d

 [65]
SCNA
(DOX/GQD)		 RG2 ≈100% with
10 µg/mL
(w/o DOX)
(alamar blue)		 λ = 808 nm
P = 2 W/cm2
t = 5 min		 DOX
2 µg/mL
AL n.r.

  • IC50 n.r.

  • ≈75% cell death with 10 µg/mL

    (alamar blue)

 Xenograft mice
(RG2 cells)
0.2 mg/mouse

  • No detectable effects

    (body weight)

 λ = 808 nm
P = 2 W/cm2
t = 10 min		 DOX
2 µg/mL
AL n.r

  • ΔT = 10 °C

  • Noticeable tumor tissue damage

    (histological)

 [8]

Table 3 abbreviations: GBNs—Graphene-based nanomaterials; GO—Graphene oxide; NGO—Nanographene oxide; rGO—Reduced Graphene oxide; GQDs—Graphene Quantum Dots; AL (wt%)—Active’s loading; d–day(s); n.r.—not reported; abl.—completely ablated; w/o—without; NIR laser– Near infrared laser; (λ, P, and t)—characteristics of the laser: wavelength; power and time; ΔT—temperature increase; IC50—concentration of GBNs required to kill 50% of cells; PTT—photothermal therapy; PDT—photodynamic therapy; AAP10—Antiarrhythmic peptide 10 (promotes bystander effect); Abs—integrin αvβ3 mAb (targeting ligand); Ag—silver; AGE-aptamer—targets melanoma inhibitor of apoptosis protein (ML-IAP) overexpressed in melanoma cells; anti-EGFR—anti-epidermal growth factor receptor (targeting ligand); APGA—amphiphilic poly-γ-glutamic acid; ArGO—rGO coated with amphiphilic poly-γ-glutamic acid; AS1411—aptamer of 26-base guanine-rich short oligonucleotide (targeting ligand); ASODN—survivin antisense oligodeoxynucleotide; Au—gold; AuNPs—gold nanoparticles; AuNRVe—gold nanorod vesicles; AuNR—Gold nanorods; AuNS—Gold nanostars; Bi2Se3—Bismuth Selenide; BHC—Berberine hydrochloride; BPEI—Branched polyethylenimine; BSA—bovine serum albumin; Ce6—Chlorin e6 (photosensitizer); cGdots—carboxylated graphene dots; Cy5.5—Cyanine 5.5 (NIR dye and photosensitizer); Cy7—Cyanine 7 (NIR dye and photosensitizer); Cys—Cysteamine hydrochloride (NIR dye); Cys-COOH—Cysteine- rich Carboxy-terminal domain CPGA—theranostic probe formed by Cy5.5 (NIR dye) labelled-matrix metalloproteinase-14 (MMP-14) substrate (CP) conjugated onto the GO/Au complex (GA); CPSS—carbon porous silica nanosheets; Cur—curcumin; DL-GQD-comp—doxorubicin hydrochloride loaded GQD complex; DOX—doxorubicin hydrochloride; DSPE—1,2-distearoyl-sn-glycero-3-phosphoethanolamine; DVDMS—bis[1-[6,7-bis[2-(sodium carbonate ethyl]-1,3,5,8,-tetramethyl-2-vinyl-porphin-4-yl]ethyl]ether (photosensitizer); FA—Folic acid (target ligand); FeCl3—Iron chloride; Fe2O3 and Fe3O4—Iron oxide nanoparticles; Gd—Gadolinium; GDH—Graphene–DOX conjugate in HA nanogel; GSPs—gold superparticles; HA—hyaluronic acid (target ligand); HA-GQD—complex of Hypocrellin A (photosensitizer), HA and GQD; HER—Herceptin, monoclonal antibody that targets HER2 Positive Metastatic Breast Cancer (target ligand); HTPGS—N-acetyl histidine-functionalized D-α-tocopherol polyethylene glycol 1000 succinate; 131I—Iodine-131 (radioisotope); ICG—NIR fluorescence dye; IO—iron oxide; IR780—IR780 iodide (NIR dye); IR-808—Heptamethine indocyanine dye (photosensitizer); LHRH—luteinizing hormone-releasing hormone peptide; Lip—Phospholipids; LOGr—low-oxygen graphene; mfHSA—multifunctional human serum albumin—HSA functionalized with indocyanine green (ICG) and lactobionic acid (LA); MMP-14(P)—Peptide substrate of MMP-14, a key endopeptidase that is overexpressed on tumor cell surface; MnWO4—manganese tungstate; MSN—mesoporous silica nanoparticles; NGR—Asn-Gly-Arg peptide that can selectively recognize CD13 isoform selectively overexpressed in tumor vasculature and certain tumor cells (target ligand); OA—Oleic acid; P—porphyrin; PAH—poly (allylamine hydrochloride); Pc—phthalocyanine; P-Cy—Cyanine 5.5 dye conjugated to GQD though a cathepsin D-responsive peptide (P); PDA or pDA—Polydopamine (reduces GO improves water solubility and biocompatibility and increases NIR absorption); PEG—Polyethylene glycol; PheoA—Pheophorbide A (photosensitizer); PLA—polylactic acid; PpIX—protoporphyrin IX (photosensitizer); PTX—Paclitaxel; PVP—polyvinylpyrrolidone; R6G—Rhodamine 6G; Res—Resveratrol; rGONM—reduced graphene oxide nanomesh; RGD—arginine–glycine–aspartic acid-based peptide (target ligand); SCNA—size-changeable graphene quantum dot nanoaircraft; SiO2 NPs—silicon dioxide nanoparticles; UCNPs—upconversion luminescence nanoparticles; ZnFe2O4—Zinc ferrite nanoparticles; ZnPc—Zinc phthalocyanine (photosensitizer); ZnS:Mn—manganese-doped zinc sulfide nanoparticles. Methods: Alamar Blue—cell proliferation assay designed to measure cell proliferation and cytotoxicity in various cell lines; Calcein AM—non-fluorescent, hydrophobic compound that easily permeates intact live cells; it can be used in a cell viability assay once, by hydrolysis, converts in calcein, a hydrophilic and strongly fluorescent compound; CCK-8—Cell Counting Kit-8 that allows sensitive colorimetric assays for the determination of cell viability in cell proliferation and cytotoxicity assays; MTT—colorimetric assay for assessing cell metabolic activity based on conversion of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide to formazan; SRB –Sulforhodamine B assay used for cell density determination, based on the measurement of cellular protein content; Trypan Blue—dye exclusion test, used to determine the number of viable cells present in a cell suspension. Cells: 4T1—mouse breast carcinoma cell line; A2780/AD—multidrug resistant human ovarian carcinoma cell line; A549—lung cancer cell line; B16F0—mouse melanoma cell line; B16F10—murine melanoma cell line; BT474—human breast cancer cell line; CHO-K1—Chinese Hamster Ovary cell line; EMT6—mouse breast cancer cell line; G361—human malignant melanoma cancer cells; H1975—lung adenocarcinoma cells; HeLa- human cervical cancer cells; HCT166—human colon cancer cells; HepG2—human hepatocellular carcinoma cell line; HT1080—human fibro-sarcoma cells; HUVEC - Human umbilical vein endothelial cells; KB—Human KB epidermal carcinoma cells; L929—mouse fibroblasts; Lewis lung—mouse lung carcinoma cells; MCF-7—human breast adenocarcinoma cell line; MCF-10—normal breast cells; MDA-MB-231—breast cancer cells; MDCK—Canine Cocker Spaniel Kidney non-cancerous cell line; MG-63—human osteosarcoma cell line; RBC—red blood cells; PC9—human adenocarcinoma cell line; RG2—mouse glioblastoma cell line; S180—murine sarcoma cancer cell line; SCC7—mouse squamous cell carcinoma cell line; SKBR-3—human epithelial breast cancer cells; U87MG—human glioblastoma astrocytoma cells; U14—mouse uterine cervical carcinoma cells; U87MG—human glioblastoma astrocytoma cells.