Formulation of amphotericin B as nanosuspension for oral administration.
Amphotherin B was formulated in a nanosuspension as a new oral drug delivery system for the treatment of experimental visceral leishmaniasis. Amphotericin B (AmB) nanosuspensions were produced by high pressure homogenisation obtaining particles with a PCS diameter of 528 nm. Environmental stability was determined in artificial gastrointestinal fluids at different pH and electrolyte concentrations. In vivo efficacy was determined in a mouse model of visceral leishmaniasis. Following oral administration (5 mg kg(-1)), micronised amphotericin B did not show any curative effect. However, administrations of amphotericin B nanosuspension, reduced liver parasite load by 28.6% compared to untreated controls.
Kayser
O
O
Freie Universität Berlin, Institut für Pharmazie, Pharmazeutische Technologie, Biopharmazie und Biotechnologie, Kelchstrasse 31, D-12169 Berlin, Germany. kayser@zedat.fu-berlin.de
Olbrich
C
C
Yardley
V
V
Kiderlen
A F
AF
Croft
S L
SL
D000284:Administration, Oral; D000666:Amphotericin B / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D000818:Animals; D002626:Chemistry, Pharmaceutical; D004195:Disease Models, Animal; D004337:Drug Carriers; D016503:Drug Delivery Systems; D004355:Drug Stability; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D007896:Leishmaniasis / Q000188:drug therapy; D008099:Liver / Q000382:microbiology; D051379:Mice; D008807:Mice, Inbred BALB C; D008854:Microscopy, Electron / Q000295:instrumentation / Q000379:methods; D008863:Microspheres; D036103:Nanotechnology; D021261:Parasitic Sensitivity Tests; D013057:Spectrum Analysis / Q000295:instrumentation / Q000379:methods; D013997:Time Factors; D014882:Water-Electrolyte Balance
D004337:Drug Carriers; D000666:Amphotericin B