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Stabilization and solubilization of difluprednate in aqueous cyclodextrin solution and its characterization for ophthalmic delivery

Stabilization and solubilization of difluprednate in aqueous cyclodextrin solution and its characterization for ophthalmic delivery


Title: Stabilization and solubilization of difluprednate in aqueous cyclodextrin solution and its characterization for ophthalmic delivery
Author: Prajapati, Manisha
Loftsson, Thorsteinn   orcid.org/0000-0002-9439-1553
Date: 2022-01
Language: English
Scope: 103106
University/Institute: Háskóli Íslands
University of Iceland
School: Heilbrigðisvísindasvið (HÍ)
School of Health Sciences (UI)
Department: Lyfjafræðideild (HÍ)
Faculty of Pharmaceutical Sciences (UI)
Series: Journal of Drug Delivery Science and Technology;69
ISSN: 1773-2247
DOI: 10.1016/j.jddst.2022.103106
Subject: Solubility; Stability; Cyclodextrins; Difluprednate; Lyfjaefnafræði; Lyfjameðferð; Skurðsjúklingar; Bólgur; Pharmaceutical chemistry
URI: https://hdl.handle.net/20.500.11815/2969

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Citation:

Manisha Prajapati, Thorsteinn Loftsson, Stabilization and solubilization of difluprednate in aqueous cyclodextrin solution and its characterization for ophthalmic delivery, Journal of Drug Delivery Science and Technology, Volume 69, 2022, 103106, ISSN 1773-2247,

Abstract:

Difluprednate is a synthetic glucocorticoid used for the treatment of postoperative inflammation and pain associated with endogenous uveitis. It is very lipophilic with limited aqueous solubility and stability. The only available marketed formulation is an oil-in-water ophthalmic emulsion that has many drawbacks. Cyclodextrin (CD) molecules are widely used to increase the solubility and stability of hydrophobic drugs through the for- mation of drug/CD complexes. This study aims to investigate degradation kinetics, stability and solubility of difluprednate in aqueous CD solutions in an effort to develop aqueous eye drop vehicle for ophthalmic delivery. Phase-solubility and kinetics studies were performed in presence of different CDs and polymers. Characterization of the drug/CD complexes was done using techniques like NMR, DSC, and FTIR. The results show that diflu- prednate has maximum stability at pH 5 in aqueous CD solution. HPγCD was found to be the best solubilizer and stabilizer among all the CDs tested. The stability was further improved with the combination of HPγCD and different polymers. Characterization of the difluprednate/HPγCD complex in solid and solution state confirmed the presence of a drug/CD complex. It was possible to solubilize 0.1% difluprednate using HPγCD and stabilize the drug using combination of CD and polymer in aqueous solution

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CC BY 4.0 © 2022 The Authors. Published by Elsevier

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