Journal of Antimicrobial Chemotherapy, Vol 42, 779-785, Copyright © 1998 by The British Society for Antimicrobial Chemotherapy
C Petit, M Cheron, V Joly, JM Rodrigues, J Bolard and F Gaboriau
Heat-induced 'superaggregation' of deoxycholate-amphotericin B (AmB- DOC,
Fungizone) was shown previously to reduce the in-vitro toxicity of this
antifungal agent. We compared AmB-DOC with the formulation obtained by
heating the commercial form (Fungizone, Bristol Myers Squibb, Paris,
France) for 20 min at 70 degrees C, in the treatment of murine infections.
An improvement of antifungal activity was obtained with heated AmB-DOC
formulations due to a lower toxicity which allowed the administration of
higher drug doses than those achievable with the commercial preparation.
Single intravenous injections of heated AmB-DOC solutions were demonstrated
to be two-fold less toxic than unheated ones to healthy mice. For mice
infected with Candida albicans, the maximum tolerated dose was higher with
heated than with unheated AmB- DOC solutions. In the model of murine
candidiasis, following a single dose of heated AmB-DOC 0.5 mg/kg, 85% of
mice survived for 3 weeks, whereas at this dose the immediate toxicity of
the standard formulation in infected mice restricted the therapeutic
efficacy to 25% survival. Both formulations were equally effective in
increasing the survival time for murine cryptococcal pneumonia and
meningoencephalitis. Injection of heated AmB-DOC solutions at a dose
two-fold higher than the maximal tolerated dose observed with the unheated
preparation (1.2 mg/kg) increased the survival time by a factor of 1.4 in
cryptococcal meningoencephalitis. These results indicate that mild heat
treatment of AmB-DOC solutions could provide a simple and economical method
to improve the therapeutic index of this antifungal agent by reducing its
toxicity on mammalian cells.
In-vivo therapeutic efficacy in experimental murine mycoses of a new formulation of deoxycholate-amphotericin B obtained by mild heating [In Process Citation]
Laboratoire de Physicochimie Biomoleculaire et Cellulaire, CNRS UA 2056, Universite P. et M. Curie, Paris, France.
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