PEGylated Graphene
Oxide as a Nanodrug Delivery Vehicle
for Podophyllotoxin (GO/PEG/PTOX) and In Vitro α‑Amylase/α-Glucosidase
Inhibition Activities
Posted on 2023-05-26 - 12:33
This study aims to develop a nanodrug delivery system
containing
podophyllotoxin (PTOX), a known anticancer drug, loaded on graphene
oxide (GO). The system’s ability to inhibit α-amylase
and α-glucosidase enzymes was also investigated. PTOX was isolated
from Podophyllum hexandrum roots with
a yield of 2.3%. GO, prepared by Hummer’s method, was converted
into GO-COOH and surface-mobilized using polyethylene glycol (PEG)
(1:1) in an aqueous medium to obtain GO-PEG. PTOX was loaded on GO-PEG
in a facile manner with a 25% loading ratio. All the samples were
characterized using FT-IR spectroscopy, UV/visible spectroscopy, and
scanning electron microscopy (SEM). In FT-IR spectral data, GO-PEG-PTOX
exhibited a reduction in acidic functionalities and there was an appearance
of the ester linkage of PTOX with GO. The UV/visible measurements
suggested an increase of absorbance in 290–350 nm regions for
GO-PEG, suggesting the successful drug loading on its surface (25%).
GO-PEG-PTOX exhibited a rough, aggregated, and scattered type of pattern
in SEM with distinct edges and binding of PTOX on its surface. GO-PEG-PTOX
remained potent in inhibiting both α-amylase and α-glucosidase
with IC50 values of 7 and 5 mg/mL, closer to the IC50 of pure PTOX (5 and 4.5 mg/mL), respectively. Owing to the
25% loading ratio and 50% release within 48 h, our results are much
more promising. Additionally, the molecular docking studies confirmed
four types of interactions between the active centers of enzymes and
PTOX, thus supporting the experimental results. In conclusion, the
PTOX-loaded GO nanocomposites are promising α-amylase- and α-glucosidase-inhibitory
agents when applied in vitro and have been reported
for the first time.
CITE THIS COLLECTION
Islam, Fawad; Khan, Farman Ali; Khan, Nasir Mehmood; Ahmad, Shujaat; Alsaiari, Ahad Amer; Almehmadi, Mazen; et al. (2023). PEGylated Graphene
Oxide as a Nanodrug Delivery Vehicle
for Podophyllotoxin (GO/PEG/PTOX) and In Vitro α‑Amylase/α-Glucosidase
Inhibition Activities. ACS Publications. Collection. https://doi.org/10.1021/acsomega.3c00888
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AUTHORS (12)
FI
Fawad Islam
FK
Farman Ali Khan
NK
Nasir Mehmood Khan
SA
Shujaat Ahmad
AA
Ahad Amer Alsaiari
MA
Mazen Almehmadi
NA
Nadeem Ahmad
ZU
Zaheer Ul-Haq
AJ
Abdul Khaliq Jan
MA
Mamdouh Allahyani
AA
Abdulaziz Alsharif
EF
Ebenezer Ola Falade
KEYWORDS
scanning electron microscopypodophyllum hexandrum rootsnanodrug delivery vehicleknown anticancer drugvisible measurements suggestedsuccessful drug loadingir spectral dataptox remained potentpegylated graphene oxideglucosidase inhibition activitiescharacterized using ftml ), respectivelyloaded go nanocomposites50 subgraphene oxidevitro visible spectroscopyptox ),loading ratioir spectroscopythus supportingsystem ’study aimsscattered typepure ptoxptox exhibitedobtain goinhibitory agentshummer ’go ).first timefacile mannerester linkagedistinct edgesaqueous mediumalso investigatedactive centersacidic functionalities3 %.