Preparation, relative toxicity and therapeutic efficacy in mice and rats of liposomal HA-1-92, a new oxohexaene polyene macrolide antibiotic.

Abstract

HA-1-92, a new polyene oxohexaene macrolide antibiotic isolated from Streptomyces CDRIL-312, was incorporated into liposomes containing phosphotidyl choline and cholesterol. The liposomal incorporated HA-1-92 considerably decreased toxicity when compared with free HA-1-92 in mice. Liposomal HA-1-92 showed improved pharmacokinetic profiles in rats. When administered to aspergillosis- and cryptococcosis-infected Balb/c mice, liposomal HA-1-92 showed increased antifungal activity, compared with free HA-1-92, with improved survival rate and decreased colony-forming units in lung, liver, spleen and kidney. These results suggest that liposomal HA-1-92 is more effective than free HA-1-92 in controlling experimental aspergillosis and cryptococcosis in Ba1b/c mice.

• Authors: J Harindran, K K Chakraborty, S R Naik
• Journal: The Journal of pharmacy and pharmacology (J Pharm Pharmacol) Vol. 51 Issue 7 Pg. 771-6 (Jul 1999) ISSN: 0022-3573 [Print] England
• PMID: 10467950 (Publication Type: Journal Article)

Chemical References

• Anti-Bacterial Agents
• HA-1-92
• Liposomes
• Macrolides

Topics

• Animals
• Anti-Bacterial Agents (adverse effects, blood, pharmacology)
• Aspergillosis (drug therapy, microbiology, mortality)
• Aspergillus fumigatus (drug effects)
• Cryptococcosis (drug therapy, microbiology, mortality)
• Cryptococcus neoformans (drug effects)
• Female
• Half-Life
• Kidney (drug effects, microbiology)
• Liposomes (chemistry)
• Liver (drug effects, microbiology)
• Lung (drug effects, microbiology)
• Lung Diseases, Fungal (drug therapy, microbiology)
• Macrolides
• Male
• Mice
• Mice, Inbred BALB C
• Muscle Tonus (drug effects)
• Rats
• Rats, Wistar
• Respiration Disorders (chemically induced)
• Spleen (drug effects, microbiology)
• Survival Rate
• Treatment Outcome