Aggregation of amphotericin B in the presence of gamma-cyclodextrin.
The macrolide antibiotic amphotericin B (AmB) forms an inclusion complex with gamma-cyclodextrin (gamma-CDx), resulting in a molecularly dispersed state of the drug. The state of aggregation of AmB in different solvents has been studied by absorption (uv-vis) and CD spectroscopy. While in aqueous solutions AmB forms colloid-like multimolecular aggregates, in the presence of gamma-CDx true solutions can be prepared, which show similar spectral properties as AmB dissolved in organic solvents. The AmB-gamma-CDx complex can be isolated as an amorphous, stable, water-soluble powder, indicating that gamma-CDx is a good carrier for the solubilization of this antibiotic. Using gamma-CDx as a carrier, the danger of precipitation of the drug during parenteral or intravenous administration can be largely reduced.
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M
Kajtár
M
M
Vikmon
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E
Morlin
J
J
Szejtli
D000666:Amphotericin B; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002942:Circular Dichroism; D003505:Cyclodextrins; D003912:Dextrins; D000431:Ethanol; D011108:Polymers; D012995:Solubility; D013057:Spectrum Analysis; D013213:Starch; D014867:Water; D047408:gamma-Cyclodextrins
D003505:Cyclodextrins; D003912:Dextrins; D011108:Polymers; D047408:gamma-Cyclodextrins; D014867:Water; D000431:Ethanol; D000666:Amphotericin B; D013213:Starch; C023792:gamma-cyclodextrin