Biodegradable microcapsules coating an anticancer drug : Experimental studies of drug release and toxicity

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In attempt to enhance anticancer effects, we produced biodegradable microcapsules with controlled release of an anticancer drug. The microcapsules were produced using the Wurster method. The core consisted of lactose and anticancer drug and was coated with membrane consisting of lecithin, cholesterol, polyvinylpyrrolidone and stearic acid. In blood plasma, the microcapsules with diameters of 90-149 m absorbed water and disintegrated in 30-60 minutes. The time required for disintegration was longer when the coating rate of the membrane was greater. Drug release : In vitro and in vivo, the drug was continuously released from the microcapsules, and drug release could be controlled by changes in the coating rate of the membrane. Effects of intra-arterial infusion : The microcapsules were injected into rabbits' renal arteries. Kidneys infused with 2mg of the biodegradable microcapsules showed little change, while kidneys infused with 2mg of non-degradable microcapsules had multiple white spotty foci, which were found to be white infarcts. When 8mg of the biodegradable microcapsules were injected, the peripheral branches of the renal arteries underwent transient occlusion, and the kidneys were found to have white spotty foci. However, infusions of 2mg repeated 4 times resulted in little damage to the renal arteries and parenchyma. These results suggest that the biodegradable microcapsules have adequate controlled release properties and are safe enough to be infused repeatedly.