Fabrication, characterization, and evaluation of microsponge delivery system for facilitated fungal therapy

Abstract

Objective: The rationale behind present research vocation was to develop and investigate a novel microsponge based gel as a topical carrier for the prolonged release and cutaneous drug deposition of fluconazole (FLZ); destined for facilitated fungal therapy.

Materials and methods: Microsponges were prepared using quasi-emulsion solvent diffusion method using Eudragit S-100. In the direction of optimization, the effect of formulation variables (drug-polymer ratio and amount of emulsifier) and diverse factors affecting physical characteristics of microsponge were investigated as well. Fabricated microsponges were characterized by differential scanning calorimetry, Fourier transform-infrared, scanning electron microscopy (SEM), particle size analysis, and also evaluated for drug content, encapsulation efficiency, in vitro drug release and in vitro antifungal activity.

Results: Compatibility studies results reflected no sign of any chemical interaction between the drug and polymers used. Whereas, varied drug-polymer ratios and emulsifier concentration indicated significant effect on production yield, drug content, encapsulation efficiency, particle size and drug release. Spherical microsponges with a porous surface and 29.327 ± 0.31 μm mean particle size were evident from SEM micrographs. In vitro release outcomes, from microsponge loaded gels depicted that F1 formulation was more efficient to give extended drug release of 85.38% at the end of 8 h, while conventional formulation by releasing 83.17% of drug got exhausted incredibly earlier at the end of 4 h merely. Moreover, microsponge gels demonstrated substantial spreadability and extrudability along with promising antifungal activity.

Conclusions: Fabricated microsponges would be impending pharmaceutical topical carriers of FLZ and a leading alternative to conventional therapy for efficient, safe and facilitated eradication of fungal infections.

Keywords: Drug delivery; fluconazole; gel; microsponges; sustained release.

Figure 1

Differential scanning calorimetry thermogram of (a) fluconazole, (b) physical mixture and (c) microsponge formulation

Figure 2

Overlain Fourier transform-infrared spectra of (a) fluconazole, (b) physical mixture and (c) optimized formulation

Figure 3

Scanning electron microscopic (a, b) and fluorescence microscopic (c, d) images of microsponges

Figure 4

X-ray diffraction patterns of (a) fluconazole and (b) microsponge formulation

Figure 5

Comparative drug release profile of (a) F1-F6, (b) F7-F10 and (c) marketed formulation

Figure 6

In vitro antifungal activity against Candida albicans

Figure 7

Drug release profile of microsponge gel during stability study