Abstract
Injectable submicron oil-in-water emulsions have important potential as a carrier for hydrophobic drugs. Conventional formulations, however, using phosphatidylcholine (PC) either with or without co-emulsifiers cannot generally be used because of their fast elimination from the blood by the reticuloendothelial system. To overcome this obstacle, we have included the amphipathic molecules of polyethylene glycol derivatives of phosphatidylethanolamine (PEG-PE) as a co-emulsifier into emulsions containing castor oil and phosphatidylcholine. Compared to the emulsions with phosphatidylcholine as the sole emulsifier or those with Tween 80 as the co-emulsifier, emulsions containing PEG-PE as a co-emulsifier of PC show a decreased liver uptake and increased blood circulation time in mice. Furthermore, they are much more stable than the conventional formulations as tested under various conditions. With superior stability and a prolonged circulation time in blood, emulsions containing amphipathic molecules of PEG may be useful for sustained release and targeted delivery of lipophilic drugs.
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