2003年5月
Cisplatin incorporated in microspheres: development and fundamental studies for its clinical application
JOURNAL OF CONTROLLED RELEASE
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- 巻
- 89
- 号
- 3
- 開始ページ
- 397
- 終了ページ
- 408
- 記述言語
- 英語
- 掲載種別
- DOI
- 10.1016/S0168-3659(03)00131-7
- 出版者・発行元
- ELSEVIER SCIENCE BV
A new drug delivery formulation, biodegradable glycolic acid-lactic acid copolymer (PGLA) microspheres incorporating cisplatin (CDDP-MS) has been developed for the treatment of peritoneal carcinomatosis. Scanning electron microscopy showed that CDDP-MS has a smooth surface and few cisplatin crystals in the hollow. An electron probe micro analyzer revealed that cisplatin was located mainly in the matrix in the state of a molecule. Release profile in vitro of CDDP from microspheres showed that the initial burst was 21.2% and the remaining CDDP was released slowly thenceforth over 14 days. Hydrolysis of CDDP-MS progresses very slowly during the 14 days, but there was no morphological change in the SEM views. The dimethylformamide content entrapped within CDDP-MS, determined by a gas chromatography, was 136 ppm at the evaporation temperature of 47 degreesC. The 50% lethal dose value of CDDP-MS, calculated by the Litchfield-Wilcoxon method, was reduced to 57% of the cisplatin solution. Therapeutic experiment on mice with peritoneal carcinomatosis showed that CDDP-MS did not enhance therapeutic effect as compared with the same dose dosage of a cisplatin aqueous solution but large quantities of cisplatin could be given in case of CDDP-MS owing to less toxicity. (C) 2003 Elsevier Science B.V. All rights reserved.
- リンク情報
- ID情報
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- DOI : 10.1016/S0168-3659(03)00131-7
- ISSN : 0168-3659
- Web of Science ID : WOS:000183088000004