engleski

Tableting of spray-dried liposomes-concept and possibilities

Liposomes, both drug loaded and empty, were prepared by the direct spray-drying of a mixture of lipid (lecithin), drug and mannitol. Metronidazole was used as model drug. Liposomes were characterized with respect to morphology, size distribution, and entrapment efficiencies before preparation of tablets. The spray-dried liposomes were mixed with mannitol (Pearlitol 100SD) and pectin (different degrees of methoxylation) or chitosan (different degrees of deacetylation) in different mixing ratios and compressed to tablets (6 mm diameter). To test tablet disintegration and evaluate liposome reconstitution, the tablets were inserted into 10 mL buffer. The properties of liposomes after reconstitution were compared to the original characteristics. The results from this study indicate the potential of tableted spray-dried liposomes. The concept may be employed for improved drug delivery through various routs of administration, e.g. the oral, buccal and vaginal route. Mucosal delivery can be achieved by application of mucoadhesive polymers in the powder mixture (outer phase) for tableting. This will result in potential in situ coating of liposomes when the tablet is disintegrated in aqueous medium. Further research is required to fully understand the new delivery system.

Dry liposomes; Soft tableting; Increased stability; Lecithin; Metronidazole

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