TY - JOUR
T1 - Neuroprotective ability of apocynin loaded nanoparticles (Apo‐nps) as nadph oxidase (nox)‐mediated ros modulator for hydrogen peroxide‐induced oxidative neuronal injuries
AU - Singh, Manisha
AU - Agarwal, Shriya
AU - Tiwari, Raj Kumar
AU - Chanda, Silpi
AU - Singh, Kuldeep
AU - Agarwal, Prakhar
AU - Kashyap, Aishwarya
AU - Pancham, Pranav
AU - Mall, Shweta
AU - Rachana, R.
AU - Sharma, Shalini
N1 - Publisher Copyright:
© 2021 by the authors. Licensee MDPI, Basel, Switzerland.
PY - 2021/8/2
Y1 - 2021/8/2
N2 - Apocynin (APO) is a known multi‐enzymatic complexed compound, employed as a via-ble NADPH oxidase (NOX) inhibitor, extensively used in both traditional and modern‐day therapeutic strategies to combat neuronal disorders. However, its therapeutic efficacy is limited by lower solubility and lesser bioavailability; thus, a suitable nanocarrier system to overcome such limitations is needed. The present study is designed to fabricate APO‐loaded polymeric nanoparticles (APO‐ NPs) to enhance its therapeutic efficacy and sustainability in the biological system. The optimized APO NPs in the study exhibited 103.6 ± 6.8 nm and −13.7 ± 0.43 mV of particle size and zeta potential, respectively, along with further confirmation by TEM. In addition, the antioxidant (AO) abilities quantified by DPPH and nitric oxide scavenging assays exhibited comparatively higher AO potential of APO‐NPs than APO alone. An in‐vitro release profile displayed a linear diffusion pattern of zero order kinetics for APO from the NPs, followed by its cytotoxicity evaluation on the PC12 cell line, which revealed minimal toxicity with higher cell viability, even after treatment with a stress inducer (H2O2). The stability of APO‐NPs after six months showed minimal AO decline in comparison to APO only, indicating that the designed nano‐formulation enhanced therapeutic efficacy for modulating NOX‐mediated ROS generation.
AB - Apocynin (APO) is a known multi‐enzymatic complexed compound, employed as a via-ble NADPH oxidase (NOX) inhibitor, extensively used in both traditional and modern‐day therapeutic strategies to combat neuronal disorders. However, its therapeutic efficacy is limited by lower solubility and lesser bioavailability; thus, a suitable nanocarrier system to overcome such limitations is needed. The present study is designed to fabricate APO‐loaded polymeric nanoparticles (APO‐ NPs) to enhance its therapeutic efficacy and sustainability in the biological system. The optimized APO NPs in the study exhibited 103.6 ± 6.8 nm and −13.7 ± 0.43 mV of particle size and zeta potential, respectively, along with further confirmation by TEM. In addition, the antioxidant (AO) abilities quantified by DPPH and nitric oxide scavenging assays exhibited comparatively higher AO potential of APO‐NPs than APO alone. An in‐vitro release profile displayed a linear diffusion pattern of zero order kinetics for APO from the NPs, followed by its cytotoxicity evaluation on the PC12 cell line, which revealed minimal toxicity with higher cell viability, even after treatment with a stress inducer (H2O2). The stability of APO‐NPs after six months showed minimal AO decline in comparison to APO only, indicating that the designed nano‐formulation enhanced therapeutic efficacy for modulating NOX‐mediated ROS generation.
KW - Antioxidant activity (AO)
KW - Cytotoxicity
KW - Reactive oxygen species (ROS)
KW - Release kinetics
KW - Transmission electron microscopy (TEM)
UR - https://www.scopus.com/pages/publications/85113285245
U2 - 10.3390/molecules26165011
DO - 10.3390/molecules26165011
M3 - Article
C2 - 34443598
AN - SCOPUS:85113285245
SN - 1420-3049
VL - 26
JO - Molecules
JF - Molecules
IS - 16
M1 - 5011
ER -