Neuroprotective Ability of Apocynin Loaded Nanoparticles (APO-NPs) as NADPH Oxidase (NOX)-Mediated ROS Modulator for Hydrogen Peroxide-Induced Oxidative Neuronal Injuries

Abstract

Apocynin (APO) is a known multi-enzymatic complexed compound, employed as a viable 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.

Transferrin-Grafted Albumin Nanoparticles for the Targeted Delivery of Apocynin and Neuroprotection in an In Vitro Model of the BBB

“…Previous results using apocynin also support our results in terms of the scavenging activity, confirming the better quenching of nitrite ions in the samples. Therefore, from the collective results, it can be concluded that cumulatively the APO-NPs showed a slightly better inhibition ability in comparison to APO alone [11]. The findings of this study demonstrate for the first time that apocynin treatments provide neuroprotection [9]…”

“…Further, a previous study showed that the intraperitoneal administration of apocynin specifically inhibits the assembly of NOX subunits (by inhibiting the translocation of the p47phox subunit from cytosol to plasma membranes) and prevented secondary BBB damage in a rat model (4 h post-blast) by restoring the dislodged tight junction proteins from the endothelial capillaries [10]. However, its therapeutic efficacy is limited by its lower solubility and bioavailability; thus, a suitable nanocarrier system to overcome such limitations is needed [11]. Drug delivery to the brain is becoming more and more important but is severely restricted by the blood-brain barrier, which severely restricts the therapy of many neurological diseases [12].…”

2-Dimensional in vitro culture assessment of ovarian cancer cell line using cost effective silver nanoparticles from Macrotyloma uniflorum seed extracts

“…In a recent review by Hembram et al (2018) , choosing AgNPs over AuNPs has been highlighted at in vivo level and can be supported by the reason of choosing Eco-friendly synthesis of AgNPs which has gained a vast recognition over globe not only because of their effectivity but also due to the efficacy ( Srivastava et al, 2018 ). Utilising the organic plant extracts in treating diseases specifically cancer is highly required considering no damage to the healthy cells which are surrounding in the tumor microenvironment ( Srivastava et al, 2018 ; Singh et al, 2021 ).…”