Session Time: 1:45pm-3:15pm
Location: Hall 3FG
Objective: In the current experimental study, we intended to develop Surface mechanized nano-formulation of naringenin (NG) as potent A(2A)AR antagonists against parkinson’s disease.
Background: One of the most common neurological problem which the world faces is Parkinson Disease (PD) associated progression, neurological degeneration and finally hampering the motor neuron with loss of drug action and expansion of disease. The need of hour is to go for novel chemicals entities in this disease. Adenosine receptors are the target molecules (A(2A)ARs) by researchers and opens different avenues in this field. Reactive oxygen or free radicals plays a significant role in pathogenesis of this disease .Naringenin (NG) is a free radical scavenger that can be used to antagonised the (A(2A)ARs) for the treatment of Parkinson Disease.
Methods: Emulsion solvent technique was employed for the development of NG loaded Nanoparticles of PLGA (NG-PLGA-NP). Drug release, particle size, poly-disparity and zeta potential were measured. Molinspiration software was used for elucidation of Lipiski’s Rule of 5. NG was subsequently appraised for invitro anti-Parkinson’s activity via free radical scavenging assay. Adenosine A2A receptor crystal structure was undertaken with the aim of selectively antagonize its effect.
Results: The prepared NG nano-formulation gave the outcome with spherical small surface with relative narrow distribution of the nanoparticles. The bioavailability of NG was in line with the Drug likeness recommendation for new entity of Chemical (NCE). It is observed that anti Parkinson activity of NG have 97% potential against DPPH free radical, respectively. NG selectively and catagorily interact with Ile80, Phe168, Ile66, Ala59, Ile274 and Tyr271 receptor at Ki ranging from 495.34nM to 5.04µM to mark adenosine A2A receptor interaction.
Conclusions: In short we can state that surface nano formulation of NG can provide some potential beneficial effect against PD by scavenging free radicals with best bioavailability.
To cite this abstract in AMA style:V. Kumar. Surface mechanised nano-formulation of naringenin as adenosine A2A receptor antagonist against in Neurological associated problem of Parkinson [abstract]. Mov Disord. 2018; 33 (suppl 2). https://www.mdsabstracts.org/abstract/surface-mechanised-nano-formulation-of-naringenin-as-adenosine-a2a-receptor-antagonist-against-in-neurological-associated-problem-of-parkinson/. Accessed December 2, 2023.
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MDS Abstracts - https://www.mdsabstracts.org/abstract/surface-mechanised-nano-formulation-of-naringenin-as-adenosine-a2a-receptor-antagonist-against-in-neurological-associated-problem-of-parkinson/