Development and characterization of oral lipid-based amphotericin B formulations with enhanced drug solubility, stability and antifungal activity in rats infected with Aspergillus fumigatus or Candida albicans

International Journal of Pharmaceutics
Ellen K WasanKishor M Wasan

Abstract

To develop an oral formulation of Amphotericin B (AmpB) with: (A) medium chain triglycerides, fatty acids and nonionic surfactants as a self-emulsifying drug delivery system (SEDDS); or (B) glyceryl mono-oleate (Peceol) with poly(ethylene glycol) (PEG)-phospholipids. SEDDS formulations were prepared by simple mixing at 40 degrees C. Peceol/DSPE-PEG-lipid formulations were prepared by solvent evaporation. Parameters evaluated included: miscibility, solubility and emulsion droplet size after incubation in simulated gastric fluid (SGF) or simulated intestinal fluid (SIF) via dynamic light scattering. The stability of AmpB in Peceol/DSPE-PEG was evaluated in SGF and SIF. Phase stability of AmpB in Peceol+/-DSPE-PEG following thermal cycling was evaluated by atomic force microscopy (AFM). Aspergillus fumigatus (2.9-3.45 x 10(7) colony forming units per mL [CFU]) or Candida albicans (3-3.65 x 10(6) CFU per mL) were injected via the jugular vein; 48 h later male albino Sprague-Dawley rats (350-400 g) were administered either a single oral gavage of a Peceol-DSPE/PEG2000-based AmpB (10 mg AmpB/kg and 5 mg AmpB/kg for the Candida albicans study only) twice daily for 2 consecutive days, a single intravenous (i.v.) dose of Abelcet (5mg Am...Continue Reading

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Citations

Jan 8, 2013·Applied Biochemistry and Biotechnology·Marina PrigolLuís Constantino
Dec 23, 2009·The Journal of Antimicrobial Chemotherapy·Pavel GershkovichKishor M Wasan
Jul 1, 2010·Therapeutic Delivery·Evren H GokceEliana B Souto
Dec 19, 2013·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Yuangang ZuKunlun Wang
Jul 23, 2013·International Journal of Pharmaceutics·T T H PhamG Barratt
Jul 19, 2014·International Journal of Pharmaceutics·Abdelkader MouriPhilippe Legrand
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Mar 20, 2019·Pharmaceutics·Ada W Y LeungMarcel B Bally
Feb 6, 2017·Drug Delivery·Min LiuZhiwen Yang

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