Page 80 - GTM-3-3

Global Translational Medicine Graphene oxide in cancer drug delivery applications

14.1%, respectively. The release of luteolin was significantly while the release rate was considerably reduced at the
higher at pH 5. The anti-cancer effect of MG and NH2-MIL- physiological pH of 7.4. 63
101(Fe)@GO@Drugs was superior compared to metal- Another study reports the synthesis of a nanocomposite
organic framework and GO alone. This enhancement was consisting of hesperidin and rGO using gamma radiation.
59
observed by the inhibition of tumor cell migration, increased Cytotoxicity studies conducted through the MTT assay
reactive oxygen species generation, and upregulation of assessed the anticancer effects of rGO on Wi38, CaCo2,
caspase-3 and caspase-9 expression. 59 and HepG2 cell lines. The results demonstrated that rGO

Fluorinated GO (FGO) was synthesized by treatment effectively inhibited the JNK/SMAD4/MMP2
functionalizing fluorinated graphene nanosheets signaling pathway, indicating its potential as a cancer
with FA pre-linked to amino-polyethylene glycol treatment.
(PEG). This modification allowed FGO to specifically An innovative nanocomposite hydrogel consisting
target cancer cells through FA receptors while also of carboxymethyl cellulose (CMC)/starch/rGO was
enhancing its solubility. The FGO-PEG-FA nanocarrier synthesized and encapsulated in double nanoemulsions
64
effectively encapsulated the anticancer drugs DOX and (Figure 1). This pH-responsive delivery system was
camptothecin, enabling their combined use for enhanced developed to effectively deliver curcumin, an antitumor
cancer treatment. Photoluminescence was applied to drug. The drug release was controlled through a water/oil/
FGO, making it an effective sensor for monitoring drug water nanoemulsion that enclosed the nanocarrier, with
loading through the inner filter effect. Moreover, near- bitter almond oil acting as the membrane. The drug loading
infrared (NIR) absorbance enabled FGO to function and entrapment efficacy were significantly improved
as a photothermal therapy (PTT) agent. The effect of compared to previously described curcumin delivery
FGO-PEG-FA on cell viability was greater than that of methods The nanocarriers exhibited pH-responsive
64
FGO, suggesting that surface modification enhances behavior, with curcumin being released more rapidly at
the biocompatibility of FGO. Minimal cytotoxicity of lower pH levels, as shown in in vitro release experiments.
both FGO-PEG-FA and FGO was observed in normal The MTT assays demonstrated elevated toxicity of the
(BEAS-2B) and cancer (HeLa) cells, even at elevated nanocomposites toward MCF-7 breast cancer cells
doses of 150 μg/mL. Under NIR irradiation, the GO compared to CMC, CMC/rGO, or free curcumin. Flow
nano-platform demonstrated significant enhancement cytometry confirmed the induction of apoptosis in
in inhibiting cancer growth, even at low dosage levels, MCF-7 cells. 64
compared to unbound DOX and control samples without
NIR irradiation. 60,61 The dimensions and configurations of different GO
preparations play distinct roles in cancer treatment. One
Nanocarriers of caffeic acid (CA) were synthesized study assessed how size and surface chemistry influence
using a hydrofluoric acid-free approach using Fe-based the in vivo behavior of graphene, significantly enhancing
metal-organic frameworks (β-CD-GO@MIL-100[Fe]) the effectiveness of graphene-based photothermal cancer
functionalized with β-cyclodextrin-conjugated GO therapy. The researchers developed nano rGO (nrGO)
(β-CD-GO) (referred to as BGw-MF). Results indicated conjugated with a non-covalent PEG coating. NRGO-
62
that BG0.5-MF exhibited the highest loading efficiency, PEG effectively targeted tumors through the enhanced
with a value of 56.44 ± 2.25% for a 2 w/w ratio of CA in permeability and retention effect. Due to significant
an alkaline environment (pH 9). In addition, the release passive tumor uptake and robust NIR absorption, nRGO-
pattern of BG0.5-MF-CA for CA was tightly regulated, PEG demonstrated remarkable efficacy as a photothermal
with approximately 57.07 ± 2.01% released at pH 5 and agent, achieving effective in vivo tumor destruction at
62
48.04 ± 1.44% at pH 7.4 over a period of 8 days. This an ultra-low laser power density of 0.15 W/cm , which
2
suggests that enhanced release in tumor regions could is significantly lower than the power densities typically
potentially improve therapeutic effectiveness. Significant employed in in vivo PTT using other nanomaterials. 65
toxicity to A549 lung cancer cells and a cell viability of In another study, four distinct types of GO were developed:
68 ± 2% were observed in in vitro cytotoxicity studies of Micrometer-sized GO (MGO; 1089.9 ± 135.3 nm),
BG0.5-MF-CA, while no evident toxicity was observed in submicrometer-sized GO (SGO; 390.2 ± 51.4 nm),
normal HEK293 cells at a dose of 400 μg/mL. 62
nanometer-sized GO (NGO; 65.5 ± 16.3 nm), and graphene
A pH-responsive drug delivery system was developed quantum dots. SGO and NGO significantly induced
63
by loading 5-fluorouracil onto GO. The formulation apoptosis, whereas MGO did not, and no detectable
exhibited controlled release of the anticancer drug at an necrosis was observed. Moreover, SGO and NGO were
acidic pH of 5.8, representative of the tumor environment, found to significantly induce autophagy. 66,67

Volume 3 Issue 3 (2024) 6 doi: 10.36922/gtm.4602