<i>In-Silico</i> Validation and Development of Chlorogenic Acid (CGA) Loaded Polymeric Nanoparticle for Targeting Neurodegenerative Disorders

Abstract

Background: Recent decades witnessed a significant growth in terms of phytocompounds based therapeutics, extensively explored for almost all types of existing disorders. They have also been widely investigated in Neurodegenerative disorders (NDDs) and Chlorogenic acid (CGA), a polyphenolic compound having potential anti-inflammatory and anti-oxidative properties, emerged as a promising compound in ameliorating NDDs. Owing to its poor stability, bioavailability and release kinetics, CGA needed a suitable nanocarrier based pharmaceutical design for targeting NDDs. Objective: The current study is aimed at the in-silico validation of CGA as an effective therapeutic agent targeting various NDDs followed by the fabrication of polymeric nanoparticles-based carrier system to overcome its pharmacological limitations and improve its stability. Methods: A successful in-silico validation using molecular docking techniques along with synthesis of CGA loaded polymeric nanoparticles (CGA-NPs) by ionic gelation method was performed. The statistical optimisation of the developed CGA-NPs was done by Box Behnken method and then the optimized formulation of CGA-NPs was characterised using particle size analysis (PSA), Transmission electron microscopy (TEM), Fourier Transform Infrared spectroscopy (FTIR) along with in-vitro release kinetics analysis. Results & Conclusion: The results attained exhibited average particle size of 101.9 ± 1.5 nm, Polydispersibility (PDI) score of 0.065 and a ZP of −17.4 mV. On a similar note, TEM results showed a size range of CGA-NPs between

Management of Brain Cancer and Neurodegenerative Disorders with Polymer-Based Nanoparticles as a Biocompatible Platform

“…The results displayed a mean size of 101.9 ± 1.5 nm with a polydispersibility of 0.065 and a ZP of −17.4 mV ( Figure 8 ). The release kinetics information from in vitro also appeared to support the release of CGA from the NPs after taking the first-order kinetics, recommending the suitable planning of nanoformulation [ 168 ].…”

“… ( a ) Graph representing the particle size analysis and ( b ) Zeta potential of the optimized nanoparticles (CGA-NPs), adapted from [ 168 ], scientific research, 2020. …”

Dietary Plant Polyphenols as the Potential Drugs in Neurodegenerative Diseases: Current Evidence, Advances, and Opportunities

“…With the development of pharmaceutics, nanoencapsulation of polymeric nanoparticles or liposomes was employed to increase the permeability across BBB and improve the bioavailability of polyphenols. For example, an in silico validation along with the synthesis of CGA-loaded polymeric nanoparticles (CGA-NPs) by ionic gelation method is developed to overcome its pharmacological limitations and improve its stability in targeting neurodegenerative diseases [452]. In addition, liposomal resveratrol exhibits a more pronounced antioxidative effect as evidenced by the radical scavenging ability and reduction in ROS production when compared to resveratrol alone [453].…”