Pongcharoenkiat N, Wirachwong P, Burananon V, Kraisintu K; International Conference on AIDS.
Int Conf AIDS. 2002 Jul 7-12; 14: abstract no. ThPeB7289.
R&D Institute, Government Pharmaceutical Organization, Bangkok, Thailand
BACKGROUND: Amphotericin B (AmB) is the drug of choice for treatment of aggressive fungal infections in AIDS victims though its severe toxicity to human still remains. Interests in developing the AmB lipid based formulations have arisen due to a number of studies indicating that AmB may be delivered to the target sites more selectively, thereby markedly reduced drug toxicity. The aim of this study was to develop the lipid-based formulation containing AmB in which the similar pattern of antifungal activity to conventional dosage form was retained while the toxicity was greatly reduced. METHODS: AmB lipid emulsions was prepared and its physicochemical properties were determined. In-vitro antifungal activity of AmB in Fungizone and in lipid emulsions was performed according to the tube dilution method. Further, cytotoxicity of AmB was studied on LLC-PK1 kidney cell lines in the MTT assay. Toxicity on human erythrocytes was also conducted to study haemolysis induced by AmB in lipid emulsions compared to that in Fungizone. RESULTS: Haemolytic activity of AmB in emulsions was markedly decreased, which was three-fold at 75 microg/ml compared with that of Fungizone at the same concentration. Cytotoxicity of the AmB in Fungizone on LLC-PK1 was found to be dose-dependent with 20 % cell survival at 100 microg/ml. No toxicity of the drug in the emulsions on cell growth was detected at any studied concentrations ranging from 20-100microg/ml. No significant differences in antifungal activity of AmB were displayed in both dosage forms. CONCLUSIONS: AmB in lipid emulsions seemed to yield a dramatic reduction in view of drug toxicity whilst the activity was retained. The tested formulation, thus, may be considered as an alternative drug delivery to the Fungizone.
Publication Types:
Keywords:
- Amphotericin B
- Antifungal Agents
- Chemistry, Pharmaceutical
- Drug Delivery Systems
- Humans
- Lipids
- Mycoses
Other ID:
UI: 102250091
From Meeting Abstracts