Formulation of Sodium Alginate Nanospheres Containing Amphotericin B for the Treatment of Systemic Candidiasis

Purpose: The aim of this work was to formulate sodium alginate nanospheres of amphotericin B by controlled gellification method and to evaluate the role of the nanospheres as a "passive carrier" in targeted antifungal therapy.
Methods: Sodium alginate nanospheres of amphotericin B were prepared by controlled gellification method, and the particle size analysis was carried out by scanning electron microscopy. The carrier capacity of sodium alginate was evaluated in terms of drug to polymer ratio. In vitro release study was carried out on all drug loaded nanospheres by the dialysis method. Release kinetics of drug from different drug loaded nanospheres was also determined. The in vivo antifungal efficacy of nanospheres bound drug vis-à-vis the free drug was evaluated in candidiasis- induced mice models.
Results: Preparation of nanospheres through controlled gellification method yielded particles with a size range of 419.6 ± 0.28 nm. Studies on drug to polymer ratio showed a linear relationship between concentration of drug and drug loading capacity. In vitro release kinetic study revealed that the release of drug from the nanospheres followed Fickian diffusion. In vivo studies showed that the nanospherebound drug produced a higher antifungal efficacy than the free drug.
Conclusion: The formulated sodium alginate nanospheres containing amphotericin B was found to have better antifungal activity when compared to the free drug and also yielded sustained in vitro release.

Keywords
Nanospheres, sodium alginate, amphotericin B, controlled gellification method, in vitro & in vivo release.