Formulation and characterization of Liposomal Fluconazole Transdermal Patch

Abstract

Introduction

Fluconazole, a prominent triazole antifungal medication, is utilized to manage a broad range of Candida infections. It has been approved by the FDA for various systemic and superficial fungal conditions, including vaginal, oropharyngeal, and esophageal candidiasis. The effectiveness of fluconazole can be significantly improved through innovative drug delivery systems.

Objectives

The main objective of this study is to develop and characterize a liposomal fluconazole transdermal patch aimed at enhancing drug delivery. This involves improving systemic absorption, reducing gastrointestinal side effects, and preventing metabolic degradation.

Methods

This research involved the development of a liposomal formulation using a thin film hydration method and its subsequent incorporation into a transdermal patch. The patch was made using a matrix composed of glycerine, gelatin, and hydroxypropyl methylcellulose (HPMC). Key parameters measured included drug content, moisture content and uptake, uniformity of weight, thickness, antifungal activity, and in-vivo drug release.

Results

The developed transdermal patches demonstrated promising pharmacokinetic properties. Key findings include: Uniformity of Weight: Patches showed high uniformity with percentages ranging from 93±0.4% to 96±0.3%. Thickness: The patches maintained consistent thickness measurements, varying from 4.1±0.03 mm to 4.3±0.04 mm. Moisture Content and Uptake: Moisture content was low, with percentages around 0.57±0.005% to 0.82±0.006%, and moisture uptake also remained under 1%. Drug Content: Drug content was robust across different formulations, ranging from 84±0.5% to 89±0.4%. In-vitro Drug Release: Drug release showed increasing absorbance over time, with significant releases observed at 30 minutes, 1 hour, and 2 hours, confirming a sustained release profile. Antifungal Activity: The patches displayed effective antifungal properties, with zones of inhibition indicating fungistatic activity against Candida albicans.

Conclusion

The liposomal fluconazole transdermal patch represents a significant advancement in antifungal medication delivery. It not only reduces the side effects associated with oral administration but also enhances bioavailability and effectiveness. The patches demonstrated a consistent and controlled release of fluconazole, improved drug content uniformity, and effective antifungal activity, making them a viable alternative to traditional fluconazole treatment methods. This innovation is expected to improve patient compliance and overall treatment outcomes for fungal infections.