[Studies on lung targeted niosomes of carboplatin].
OBJECTIVE
To improve the treatment efficacy and reduce the side effect of carboplatin (CBP), the antitumor drug was incorporated into niosomes (NS).


METHODS
Lung targeted niosomes of CBP (CBP-NS) were prepared by the method of hand shaking. The ultraviolet absorption spectrophotometric method was used for the determination of CBP. The method of dynamic dialysis was used for in vitro release of CBP from CBP-NS. The S-180 lung neoplasms models were established by i.v. cancer cells in mice. The number of pulmonary nodules was examined for evaluating the therapeutic efficacy.


RESULTS
The data showed that the mean diameter of CBP-NS was 3.72 microns, with a span of 0.66. The entrapment ratio of CBP in CBP-NS was 29.2% and the CBP-NS were stable for three months stored at 3 degrees C-5 degrees C, 15 degrees C-25 degrees C or 37 degrees C (relative humidity 75%). The release profile in vitro could be described by a biexpotential equation. The calculated values of the three targeting parameters indicated that CBP-NS showed good targeting efficiency. The results of therapeutic trials showed that the antitumor effects were significantly increased by injection of CBP-NS compared with CBP in the treatment of mice with lung carcinoma.


CONCLUSIONS
The results indicated that CBP-NS have good targeting efficiency in vivo, and the biodegradable CBP-NS may decrease the side effects of carboplatin and improve its therapeutic efficacy.
Zhang
J Q
JQ
School of Pharmacy, West China University of Medical Sciences, Chengdu 610041, China.
Lu
B
B
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D016190:Carboplatin / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D004337:Drug Carriers; D016503:Drug Delivery Systems; D005260:Female; D008168:Lung / Q000378:metabolism*; D008175:Lung Neoplasms / Q000188:drug therapy; D051379:Mice; D011897:Random Allocation; D013501:Surface-Active Agents
D000970:Antineoplastic Agents; D004337:Drug Carriers; D013501:Surface-Active Agents; D016190:Carboplatin