Amphiphilic association systems for Amphotericin B delivery.
The present study describes the production and characterization of amphiphilic association systems for Amphotericin B (AMB). In particular, three different classes of microemulsions and different monoglyceride-water systems were produced. Formulations were characterized for macroscopic aspect, pH, rheology, mean size and size distribution, both in the absence and in the presence of AMB. AMB solubility was investigated in the different formulations by HPLC studies. The formulations increased AMB solubility up to 20-fold with respect to the single oil and aqueous phases employed for microemulsion production.AMB diffusion studies from two microemulsions taken as models were performed in a Franz cell system using a nylon membrane. The physical and chemical stability of AMB-containing amphiphilic association systems were investigated for three months after production. For physical stability studies both the macroscopic aspect, droplet mean size and dimensional distribution were analysed. For chemical stability studies, the AMB content of the formulations was quantified by HPLC analysis. Microemulsions and monoglyceride-water systems were free from phase separation for up to three months and in some cases the AMB content was unchanged even after three months.
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Dipartimento di Scienze Farmaceutiche, Università di Ferrara, via Fossato di Mortara, 19, I-44100 Ferrara, Italy. ese@unife.it
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D000287:Administration, Topical; D000666:Amphotericin B / Q000008:administration & dosage / Q000737:chemistry*; D000935:Antifungal Agents / Q000008:administration & dosage / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D004058:Diffusion; D004355:Drug Stability; D004655:Emulsions; D005989:Glycerides / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D010316:Particle Size; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D014783:Viscosity; D014867:Water / Q000737:chemistry
D000935:Antifungal Agents; D004655:Emulsions; D005989:Glycerides; D013501:Surface-Active Agents; D014867:Water; D000666:Amphotericin B