Lung-targeting microspheres of carboplatin

Abstract

Carboplatin (CPt) was incorporated in the gelatin microspheres by the method of emulsion and the drug content determined spectrophotometrically. The arithmetic mean diameter of the microspheres was 13.20 μm with 98% of the microspheres ranging from 5.0 to 28.6 μm. The average carboplatin content was 23.76% and the yield of the microspheres 85.12%. The microspheres were stable for three months when stored at 37 °C/RH 75%, showing insignificant change in appearance and drug content. The in vitro release profile of the microspheres could be described by a biexponential equation, and the release t 1/2 was 49.7 min and 92.04% released in 10 h; while for the original drug, CPt, under the same conditions, 92.15% released in the first half an hour. Very high lung-targeting efficiency in vivo was proved by the results of targeting parameters. The S-180 lung neoplasm models were established by i.v. cancer cells in mice and the number of pulmonary nodules examined for evaluation of the treatment effect. The results of therapeutic tests showed that the antitumour effects were increased by injection of the microspheres compared with the injection of CPt solution: half of the dose in the microspheres showed comparable effect to the original drug.