Abstract:
Amphotericin B (AmB), is an effective antifungal and anti leishmenial agent associated with low oral bioavailability which is available in liposomal and simple preparation intended for parenteral administration. Simple AmB preparations are associated with relatively high toxicity and high cost of liposomal formulations necessitate the development of economical, safe and novel AmB formulation. The advancement in nanotechnology has equipped the formulator with sophisticated instruments and now the stability related features of macro and colloidal dispersion are optimized by characterizing the micro and nanoparticles present in the formulation. In this study we have developed emulsion based AmB preparation using canola oil with low surfactant concentration. AmB was dispersed in in HPMC solution oil was emulsified with the help of tween 80 and carbopol. The prepared emulsion was characterized for stability and in vitro antifungal and anti leishmenial activity. The size, shape and elemental composition of entrapped particles was determined through scanning electron microscopy (SEM), energy dispersive x-ray spectrometry (EDS) and optical microscopy and wider range particle of spherical shape were observed in oven dried emulsion. However the freeze dried sample showed the particle of less than 100 nm in diameter. Thin layer chromatography (TLC) based assay confirmed the intactness of AmB in prepared emulsion. AmB emulsion showed the comparable antifungal activity against Aspergillus fumigatus, Aspergillus flavus, Aspergillus niger and Fusarium solani when tested. In vitro anti leishmenial assay showed that AmB emulsion having 0.2µg/ml was able to kill 50% of organism and 100 % mortality was observed with emulsion containing 20µg/ml. This study aims about preparation of AmB formulation, O/W emulsion utilizing HPMC and carbopol viscosity enhancing agent to improve the stability of nano and micronized globules produced during the emulsification process.
