Abstract
In the current study, the effect of poloxamer 188 on the complexation efficiency and dissolution of arbidol hydrochloride (ADL), a broad-spectrum antiviral agent, with β-cyclodextrin (β-CD) was investigated. Phase solubility studies confirmed a stoichiometry of a 1:1 ratio for both ADL:β-CD and ADL/β-CD with a 1% poloxamer 188 system with an AL type of phase solubility curve. The stability constants (K1:1) calculated from the AL type diagram were 550 M-1 and 2134 M-1 for AD:β-CD and ADL/β-CD with 1% poloxamer 188, respectively. The binary ADL/β-CD and ternary ADL/β-CD with 1% poloxamer 188 complexes were prepared by kneading and a solvent evaporation method and were characterized by aqueous solubility, FTIR, PXRD, DSC and SEM in vitro studies. The solubility (13.1 fold) and release of ADL were markedly improved in kneaded ternary ADL/β-CD with 1% poloxamer 188 (KDB). The binding affinity of ADL and β-CD was confirmed by 1H NMR and 2D ROSEY studies. The ternary complex (KDB) was further subjected for in vivo pharmacokinetic studies in rats and a significant improvement in the bioavailability (2.17 fold) was observed in comparison with pure ADL. Therefore, it can be concluded that the solubilization and bioavailability of ADL can be remarkably increased by ADL/β-CD complexation in the presence of a third component, poloxamer 188.
Highlights
Arbidol hydrochloride (ADL), known as umifenovir, is a Russian-made potent broad-spectrum antiviral agent
ADL is used for prophylaxis as well as the treatment of human pulmonary diseases caused by influenza A and B viruses, hepatitis C and other human pathogenic respiratory viruses [1,2,3]
It was revealed from the data that the addition of 1% poloxamer 188 to β-CD enhanced the interaction of ADL with β-CD by increasing the stability constant
Summary
Arbidol hydrochloride (ADL), known as umifenovir, is a Russian-made potent broad-spectrum antiviral agent. With the improvement of ADL solubility, it would be possible to obtain formulations with low doses, a reduced dose frequency and better compliance access of the medicine Owing to their non-toxic nature and complexation ability, a cyclodextrins (CDs)-based drug delivery system is commonly employed as a promising platform to increase drug solubility and stability, which enhances the drug release profile [14]. In this context, the inclusion complexes of poorly water soluble drugs with α-cyclodextrin, β-cyclodextrin and γ-cyclodextrin are widely reported in the literature [15,16]. We report the preparation and characterization of β-cyclodextrin-ADL (ADL/β-CD) complexes with 1% poloxamer 188 in order to improve the solubilization and bioavailability properties
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