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  • Title: Long-term stability of sterically stabilized liposomes by freezing and freeze-drying: Effects of cryoprotectants on structure.
    Author: Stark B, Pabst G, Prassl R.
    Journal: Eur J Pharm Sci; 2010 Nov 20; 41(3-4):546-55. PubMed ID: 20800680.
    Abstract:
    Liposomes are widely investigated for their use as drug delivery systems, where they have to meet strict stability criteria. Hence, it is of common interest to establish appropriate storage conditions to improve the shelf life of liposomes. In general, long-term stability can be achieved by freezing as well as freeze-drying, and different carbohydrates or polyalcohols, such as mannitol or glycerol are considered as cryoprotective agents to inhibit liposomal fusion or degradation during freezing procedures. Here, we determined the impact of different cryoprotectants on physicochemical parameters of sterically stabilized PEGylated liposomes, which become increasingly important for pharmaceutical applications. We investigated particle stability in terms of size, lamellarity and thickness of the lipid bilayer using photon correlation spectroscopy and small angle X-ray scattering. Besides, we evaluated the impact of cryoprotectants on the thermal lipid phase behavior of either frozen/thawn or lyophilised/rehydrated PEGylated liposome formulations by differential scanning calorimetry. Optimal results for the preservation of the average size of the extruded unilamellar liposomes during freezing were achieved using a mixture of glycerol and carbohydrate concentrations of about 1% (w/v), irrespective of the carbohydrate used. We found no significant changes in the bilayer organisation, and the transition behavior of lipids was almost uneffected by freezing. In case of freeze-drying, similar carbohydrate concentrations as used for freezing were sufficient to maintain the size of PEGylated liposomes after reconstitution of the dried lyophilised cakes, but our small angle X-ray scattering data provide strong evidence that the lyophilisation/rehydration process affects lipid membrane reorganisation on a molecular level such that a swelling of the bilayer might occur. These internal structural changes, which are not detected by standard particle size analysis, might well influence drug release profiles and the pharmacological performance of a liposomal drug delivery system.
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