Effects of glucose and its oligomers on the stability of freeze-dried liposomes

Abstract

The effects of glucose and its oligomers (maltodextrins) on the stability of sonicated liposomes during freeze-drying were studied by monitoring the retention of the fluorescent dye, Calcein, entrapped in the liposomal inner aqueous phase and by the use of differential scanning calorimetry (DSC). Glucose showed weak cryoprotective effects on dioleoylphosphatidylcholine (DOPC) or egg yolk phosphatidylcholine (eggPC) liposomes, while it had a relatively high cryoprotective effect on dipalmitoylphosphatidylcholine (DPPC) liposomes. Maltose and maltotriose showed high cryoprotective effects on eggPC liposomes, while other maltodextorin, longer oligomers, showed low cryoprotective effects. No saccharide was effective to protect DOPC liposomes. The fluidity and/or packing of lipid membranes had considerable influences on the stability of liposomes during the lyophilization. Maltodextrins showed relatively high cryoprotective effects on DPPC liposomes at low saccharide/lipid molar ratios, although the cryoprotective effects decreased with the increase in the molar ratios. Size measurements suggested that glucose and maltose completely prevented the aggregation and/or fusion of liposomes during lyophilization, and that other maltodextrins induced them due to their weak hydrophobic properties.