Self-nanomicellizing solid dispersion of edaravone: part I - oral bioavailability improvement

Drug Design, Development and Therapy
Ankit ParikhXin-Fu Zhou

Abstract

Edaravone (EDR) is known for its free radical scavenging, antiapoptotic, antinecrotic, and anticytokine effects in neurological and non-neurological diseases. It is currently available clinically as Radicava® and Radicut®, intravenous medications, recently approved for the treatment of amyotrophic lateral sclerosis and cerebral infarction. However, the oral use of EDR is still restricted by its poor oral bioavailability (BA) due to poor aqueous solubility, stability, rapid metabolism, and low permeability. The present study reports the development of novel EDR formulation (NEF) using self-nanomicellizing solid dispersion (SNMSD) strategy with the aim to enable its oral use. The selection of a suitable carrier for the development of NEF was performed based on the miscibility study. The optimization of EDR-to-carrier ratio was conducted via kinetic solubility study after preparing SNMSDs using solvent evaporation technique. The drug-polymer carrier interaction and self-nanomicellizing properties of NEF were investigated with advanced characterization studies. In vitro permeation, metabolism, and dissolution study was carried out to examine the effect of the presence of a carrier on physico-chemical properties of EDR. Additionally...Continue Reading

Citations

Jul 31, 2020·Pharmaceutical Development and Technology·Liyan ZhaoYiling Wu
Jan 31, 2020·Journal of Neuropathology and Experimental Neurology·Erwin A van VlietEleonora Aronica
Jul 16, 2020·Advanced Pharmaceutical Bulletin·Avinash Ramrao Tekade, Jyoti Narayan Yadav
Mar 1, 2020·Journal of Controlled Release : Official Journal of the Controlled Release Society·Delaram BabadiAzadeh Haeri

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Methods Mentioned

BETA
Protein Assay
Differential
X-ray
nuclear magnetic resonance
transmission electron microscopy
NMR

Software Mentioned

SOL
Phoenix WinNonlin
GraphPad Prism
Image Analysis
Topspin

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