Preparation and evaluation in vitro and in vivo of polylactic acid microspheres containing doxorubicin.

Abstract
Polylactic acid microspheres containing doxorubicin [anticancer drug] were prepared by a solvent-evaporation process and release patterns of the drug from the microspheres were examined in vitro. Microspheres with greater drug counts released more drug. The release rate of the drug after the initial burst was small, so that prolonged release was obtainable. The wettability of the microspheres might influence the release rate. Venous plasma levels of the drug following intra-arterial administration into dog liver were considerably lower than those following administration of the drug solution. Microangiography revealed embolization due to the micropheres in peripheral arteries in the liver.