Lung-targeting microspheres of carboplatin.
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 microm with 98% of the microspheres ranging from 5.0 to 28.6 microm. 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 degrees 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 10h; 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.
Lu
B
B
West China School of Pharmacy, Sichuan University, #17, 3rd Block, Renmin South Road, Chengdu 610041, China. lubin@wcums.edu.cn
Zhang
J Q
JQ
Yang
H
H
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use / Q000633:toxicity; D001682:Biological Availability; D016190:Carboplatin / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use / Q000633:toxicity; D016503:Drug Delivery Systems; D004355:Drug Stability; D005260:Female; D007275:Injections, Intravenous; D007928:Lethal Dose 50; D008168:Lung / Q000187:drug effects / Q000378:metabolism*; D008175:Lung Neoplasms / Q000188:drug therapy / Q000378:metabolism*; D051379:Mice; D008863:Microspheres; D009368:Neoplasm Transplantation; D010316:Particle Size; D014018:Tissue Distribution
D000970:Antineoplastic Agents; D016190:Carboplatin