Mannosylated Liposomes as Carriers for Hamycin in the Treatment of Experimental Aspergillosis in Balb/C Mice

Abstract

Hamycin incorporated into mannosylated liposomes produced less toxicity and enhanced antifungal activity in experimental aspergillosis in balb/c mice in vivo. Incorporation of cholesterol into mannosylated liposomes led to a decrease in hamycin toxicity. The LD₅₀ (mg/kg) values of hamycin contained in SPC/Chol/DPPE-Man (molar ratio 4:5:1) lipsomes was 2.8 whereas that in SPC/DPPE-Man liposomes (molar ratio 9:1) was 1.4. Incorporation of cholesterol into mannosylated liposomes increased the survival rates of infected animals: 70% survival was recorded after 7 days therapy as well as reduced fungal load in lung, liver, spleen and kidney. HPLC studies of distribution of hamycin in various tissues showed a reduction in the concentration of the liposomal drug in circulation compared to that observed for free drug and neutral liposomes after 1 hour.

Key Words:

• Aspergillosis
• Hamycin
• Mannosylated liposomes
• Reticuloendothelial System