Role of Polymer Type and Ratio in Improving the Solubility of Voriconazole Solid Dispersion: A Comparative Study
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Author:
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SAJAD MONEIM HAKEEM, ATHMAR DAHIR HABEEB, GAITH ALI JASIM
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Abstract:
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Fungal keratitis is an infection of the cornea of the eye that often requires the use of antifungal drugs. Antifungal eye drops use is limited due to low solubility of the antifungal drugs and rapid elimination of instilled eye drops. The aim of our research is to increase the solubility of poorly soluble drug voriconazole using solid dispersion to be used as an antifungal eye treatment. The current study investigates the effect of different types and ratios of polymers on the properties of the prepared solid dispersion. Solid dispersion was fabricated by the solvent evaporation method at a drug: polymer ratios of (1:1, 1:3, 1:5, 1:7 and 1:9) using three different polymers; Soluplus®, Poloxamer 188 and Poloxamer 407. The formulations were compared regarding their saturated solubility. Formula 14, which has 1:7 drug:Soluplus® ratio, showed the most promising results regarding improving solubility and was further tested for dissolution. The amorphous state of the drug due to solid dispersion was examined using XRD and DSC, and the results demonstrated a conversion from crystalline to the amorphous state. The solubility of voriconazole was significantly improved using solid dispersion and has the potential to be used as eye formulation for the treatment of fungal keratitis.
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Keyword:
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Solid dispersion, Soluplus®, Voriconazole, Solubility.
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EOI:
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DOI:
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https://doi.org/10.31838/ijpr/2020.12.01.343
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