ENHANCING FLUCONAZOLE SOLUBILITY AND BIOAVAILABILITY THROUGH SOLID DISPERSION TECHNIQUES: EVALUATION OF POLYETHYLENE GLYCOL 6000 AND SODIUM CARBOXYMETHYLCELLULOSE SYSTEMS USING FIBER

WAFA SULAIMAN AL HATTALI; BETTY ANNIE SAMUEL; ANIL K. PHILIP

doi:10.22159/ijpps.2024v16i12.52739

Authors

WAFA SULAIMAN AL HATTALI School of Pharmacy, College of Health Sciences, University of Nizwa, Birkat Al Mouz-616, Nizwa, Oman
BETTY ANNIE SAMUEL School of Pharmacy, College of Health Sciences, University of Nizwa, Birkat Al Mouz-616, Nizwa, Oman
ANIL K. PHILIP School of Pharmacy, College of Health Sciences, University of Nizwa, Birkat Al Mouz-616, Nizwa, Oman https://orcid.org/0000-0003-2960-330X

DOI:

https://doi.org/10.22159/ijpps.2024v16i12.52739

Keywords:

Bioavailability, Dissolution rate, Fluconazole, PEG 6000, Solid dispersion, Solubility enhancement

Abstract

Objective: The triazole antifungal fluconazole is widely used for treating mycotic infections, but its efficacy is limited by its poor aqueous solubility and low dissolution rate, leading to reduced oral bioavailability. This study aimed to enhance the solubility and dissolution rate of fluconazole using solid dispersion techniques with Polyethylene Glycol 6000 (PEG 6000) and Sodium Carboxymethylcellulose (SCMC) as carriers.

Methods: Solid dispersions were prepared using the fusion method, and their physicochemical properties were evaluated against physical mixtures and pure drug samples.

Results: The solid dispersion showed a significant increase in the dissolution rate, achieving 89.01% drug release in 180 minutes compared to 40.3% for the pure drug (p < 0.0032) and 84.1% for the physical mixture (p < 0.0453). The encapsulation efficiency of the solid dispersion was 39.24%, with a drug loading capacity of 19.62%. Fourier Transform Infrared (FTIR) spectroscopy confirmed the stability of the drug within the dispersion, while Scanning Electron Microscopy (SEM) revealed amorphous particles, indicating enhanced solubility.

Conclusion: These results demonstrate that the solid dispersion of fluconazole with PEG 6000 and SCMC significantly improves its dissolution rate and flow properties, providing a promising strategy for enhancing the oral bioavailability of poorly water-soluble drugs.

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