Next Article in Journal
New Acyl Derivatives of 3-Aminofurazanes and Their Antiplasmodial Activities
Next Article in Special Issue
Guest-Mediated Reversal of the Tumbling Process in Phosphorus-Dendritic Compounds Containing β-Cyclodextrin Units: An NMR Study
Previous Article in Journal
Role of Citicoline in the Management of Traumatic Brain Injury
Previous Article in Special Issue
Implementation of an Enzyme Membrane Reactor to Intensify the α-O-Glycosylation of Resveratrol Using Cyclodextrins
Article

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

1
Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi Arabia
2
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh P.O. Box 2457, Saudi Arabia
3
Bioavailability Unit, Central Laboratory, College of Pharmacy, King Saud University, Riyadh P.O. Box 2457, Saudi Arabia
4
Department of Pharmacology, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi Arabia
5
Department of Pharmaceutics and Central Lab, College of Pharmacy, King Saud University, Riyadh P.O. Box 2457, Saudi Arabia
*
Author to whom correspondence should be addressed.
Academic Editors: Laura Catenacci, Milena Sorrenti and Maria Cristina Bonferoni
Pharmaceuticals 2021, 14(5), 411; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050411
Received: 9 March 2021 / Revised: 16 April 2021 / Accepted: 21 April 2021 / Published: 26 April 2021
(This article belongs to the Special Issue New Frontiers in Cyclodextrin Technologies)
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. View Full-Text
Keywords: arbidol; β-cyclodextrin; poloxamer 188; ternary complex; solubilization; bioavailability arbidol; β-cyclodextrin; poloxamer 188; ternary complex; solubilization; bioavailability
Show Figures

Figure 1

MDPI and ACS Style

Anwer, M.K.; Iqbal, M.; Ahmed, M.M.; Aldawsari, M.F.; Ansari, M.N.; Ezzeldin, E.; Khalil, N.Y.; Ali, R. Improving the Solubilization and Bioavailability of Arbidol Hydrochloride by the Preparation of Binary and Ternary β-Cyclodextrin Complexes with Poloxamer 188. Pharmaceuticals 2021, 14, 411. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050411

AMA Style

Anwer MK, Iqbal M, Ahmed MM, Aldawsari MF, Ansari MN, Ezzeldin E, Khalil NY, Ali R. Improving the Solubilization and Bioavailability of Arbidol Hydrochloride by the Preparation of Binary and Ternary β-Cyclodextrin Complexes with Poloxamer 188. Pharmaceuticals. 2021; 14(5):411. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050411

Chicago/Turabian Style

Anwer, Md. K., Muzaffar Iqbal, Mohammad M. Ahmed, Mohammed F. Aldawsari, Mohd N. Ansari, Essam Ezzeldin, Nasr Y. Khalil, and Raisuddin Ali. 2021. "Improving the Solubilization and Bioavailability of Arbidol Hydrochloride by the Preparation of Binary and Ternary β-Cyclodextrin Complexes with Poloxamer 188" Pharmaceuticals 14, no. 5: 411. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050411

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop