Improving the Solubilization and Bioavailability of Arbidol Hydrochloride by the Preparation of Binary and Ternary β-Cyclodextrin Complexes with Poloxamer 188

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.

Formulation of Genistein-HP β Cyclodextrin-Poloxamer 188 Ternary Inclusion Complex: Solubility to Cytotoxicity Assessment

“…Anwer et al formulated a ternary inclusion complex of Arbidol hydrochloride using β CD with ternary substance poloxamer 188. The dissolution result revealed 94.5% drug release in the tested 1 h [24]. Our dissolution results also showed a similar type of result using PL 188 as ternary substance.…”

“…Arbidol hydrochloride using poloxamer 188 and showed better stability constan 2134 M −1 [24]. The findings of our study were found to be greater than the bina and similar to the ternary systems.…”

“…and the result showed the stability constant value of 10.9 M −1 which is less than o oped GS-TC [35]. In another study, Anwer et al formulated ternary inclusion c Arbidol hydrochloride using poloxamer 188 and showed better stability constan 2134 M −1 [24]. The findings of our study were found to be greater than the bina and similar to the ternary systems.…”

“…It contains two hydrophilic parts which are linked with the lipophilic part. It has good surfactant properties and is commonly used for solubility enhancement of poorly soluble drugs [23,24].…”

Design of Olmesartan Medoxomil-Loaded Nanosponges for Hypertension and Lung Cancer Treatments

“…Moreover, in another study, we demonstrated that butenafine-loaded NSs could enhance the therapeutic efficacy through channeling the drug deeper into the skin layers at the target site to completely eradicate fungal infections [ 15 ]. In addition, starch derivatives and especially, cyclodextrin-based NSs have recently emerged due to the excellent properties owing to their distinct structure [ 16 , 17 ].…”