Design and Development of Fluconazole-Loaded Nanocellulose-Eudragit Vaginal Drug Delivery System

Purpose

The purpose of this research work was to evaluate the scaffolds of rice and wheat nanocellulose with Eudragit E100 for vaginal delivery of fluconazole.

Method

The nanocellulose-based scaffolds were fabricated by the lyophilization technique using a two-factor three-level central composite experimental design. The optimal formulation of the fluconazole-loaded Eudragit-coated rice or wheat nanocellulose-based scaffolds comprised of nanocellulose (3.4% w/v or 3.3% w/v) and Eudragit E100 (6.3% w/v or 7.9% w/v), respectively.

Results

The Fourier-transform infrared spectroscopy confirmed the Eudragit coating on nanocellulosic fibers while the thermogravimetric study unveiled the higher thermal stability of coated scaffolds. The diffraction pattern and electron micrographs revealed the amorphous and porous nature of the fabricated scaffolds. The molecular weight of rice and wheat nanocellulose-based scaffolds was determined to be 9.7 × 10⁶ Da and 6.07 × 10⁶ Da, respectively, by the static light scattering. Further, the Eudragit-coated nanocellulose scaffolds show greater swelling (fivefold higher), porosity (> 84%), tensile strength (> 274 MPa), and mucoadhesive strength (> 1940 mN), and less enzymatic degradation rate over the unmodified scaffolds. The optimal batch of Eudragit-coated nanocellulose scaffolds provided a sustained release of 99% of fluconazole over 48 h with 1.12-fold higher ex vivo vaginal permeation over the native scaffolds. In addition, the Eudragit-coated wheat nanocellulose-based scaffolds were found to be antifungal and non-cytotoxic in nature.

Conclusion

The research work demonstrates that fluconazole-loaded Eudragit-coated rice or wheat nanocellulose scaffolds can be utilized as a vaginal drug delivery system.