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Optimizing Mucoadhesive Film-Forming Spray for Efficient Oral Delivery of Fluconazole in Candidiasis Treatment
Ilaf J Atoosh1, Mowafaq M Ghareeb2
1Department of Pharmacy, Ministry of Health and Environment, Baghdad, IRQ.
Abstract:
Buccal candidiasis has become increasingly prevalent in recent years, with Candida albicans being the primary causative organism. While systemic fluconazole is an effective treatment, its use is associated with adverse effects such as gastric upset, hepatic failure, and potential drug interactions. Therefore, the development of local fluconazole treatment presents a promising solution to these challenges. This study aimed to formulate an efficient local mucoadhesive film-forming spray for the targeted delivery of fluconazole in the treatment of oral candidiasis. The investigation involved the use of three polymers (hyaluronic acid, polyvinyl alcohol, and xanthan gum) both individually and in combination to identify the most effective formulation. Various tests were conducted to characterize 13 formulations prepared using these polymers, including UV-vis spectroscopy, Fourier-transform infrared spectroscopy (FTIR), content assay, drying time and film formation, viscosity determination, determination of the mucoadhesion strength by turbidimetric methods, drug release study, in-vitro anticandida activity, histological irritation analysis, and stability study. The optimum formula F11, comprised polyvinyl alcohol for its superior mechanical properties and film-forming capabilities, hyaluronic acid, and xanthan gum in combination, exhibiting synergistic mucoadhesive strength. This optimal formulation demonstrated maximum mucoadhesion, rapid film formation, an acceptable spray angle, and controlled release. Furthermore, the optimum formula underwent additional evaluations for in vitro anti-Candida activity, in vivo irritancy assessments, and stability studies, all of which yielded satisfactory results. These findings support the potential of the optimum formula as a straightforward and efficient spray formulation for the treatment of oral candidiasis.
Insights
A novel mucoadhesive spray formulation for local fluconazole delivery effectively treats oral candidiasis. This innovative approach minimizes systemic side effects associated with oral antifungal medications.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Mycology
Background:
- Buccal candidiasis is a growing concern, often caused by Candida albicans.
- Systemic fluconazole is effective but carries risks of adverse effects and drug interactions.
- Local drug delivery offers a promising alternative for treating oral fungal infections.
Purpose of the Study:
- To formulate and characterize a mucoadhesive film-forming spray for targeted local delivery of fluconazole.
- To evaluate the efficacy of the spray formulation in treating oral candidiasis.
- To identify optimal polymer combinations for enhanced mucoadhesion and drug release.
Main Methods:
- Formulation of 13 different mucoadhesive sprays using hyaluronic acid, polyvinyl alcohol, and xanthan gum.
- Characterization of formulations via UV-vis spectroscopy, FTIR, content assay, drying time, viscosity, mucoadhesion strength, and drug release studies.
- Evaluation of in vitro anti-Candida activity, in vivo irritancy, and stability of the optimized formulation.
Main Results:
- The optimal formulation (F11) combined polyvinyl alcohol, hyaluronic acid, and xanthan gum, demonstrating synergistic mucoadhesive strength.
- F11 exhibited rapid film formation, acceptable spray characteristics, and controlled drug release.
- In vitro and in vivo studies confirmed the anti-Candida efficacy and safety of the optimized spray.
Conclusions:
- The developed mucoadhesive film-forming spray provides an efficient and targeted delivery system for fluconazole in treating oral candidiasis.
- This local delivery approach offers a safer alternative to systemic antifungal treatments.
- The optimized formulation shows significant potential for clinical application in managing oral fungal infections.
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