The effect of lipid composition upon the encapsulation and in vitro leakage of metaproterenol sulfate from 0.2μm diameter, extruded, multilamellar liposomes

Abstract We have investigated the encapsulation and permeability properties of sucrose and metaproterenol sulfate in 0.2 μm diameter, multilamellar vesicles having forty different liposomal lipid compositions. Whereas sucrose showed no detectable leakout under the in vitro conditions employed, metaproterenol sulfate exhibited α 340-fold range in efflux half-life times. This range could be correlated with recognized formulation variables, such as phospholipid fatty acid composition (including chain length and degree of unsaturation), vesicle charge, and presence of cholesterol. The data presented may be useful in selecting liposome formulations of water-soluble drugs having desired release characteristics for controlled drug delivery.

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