Studies on pharmaceutical modification of anticancer agents. II. Enhanced delivery of bleomycin into lymph by emulsions and drying emulsions.

Abstract

The enhanced delivery into lymph of bleomycin was studied by i.p. and i.m. injection of oil emulsified preparations. A comparison of concentration of bleomycin in thoracic duct lymph showed that W/O [water in oil] emulsion was the most effective and followed by O/W [oil in water] emulsion. An application of spray drying powder was also attempted to enhance delivery, and the lymph concentration was increased as compared with injection of the aqueous solution, although lower than with O/W liquid emulsion. A measuring of binding to oil particles indicated that .apprxeq. 40% of bleomycin was bound to the particles of O/W liquid emulsion and reconstituted emulsions prepared from drying products. The clearance rates of bleomycin from the muscle were delayed by about 1/2 by W/O, O/W and reconstituted emulsion. The possible mechanism of enhanced delivery into rat lymph was discussed.