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Phthalimide polymers of camptothecin

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Attachment of anticancer agents to polymers has been demonstrated to improve their therapeutic profiles. A new monomer containing camptothecin, 5‐norbonene‐endo‐2,3‐dicarboxylimidoundecanoyl‐camptothecin (NDUCPT) and its homopolymer and copolymer with acrylic acid (AA) were synthesized and spectroscopically characterized. The NDUCPT content in poly(NDUCPT‐co‐AA) obtained by elemental analysis was 51%. The average molecular weights of the polymers determined by gel permeation chromatography were as follows: M n = 12 100, M w = 23 400 g mol−1, M w/M n = 1.93 for poly(NDUCPT), M n = 15 400, M w = 28 300 g mol−1, M w/M n = 1.83 for poly(NDUCPT‐co‐AA). The IC50 value of NDUCPT and its polymers against U937 cancer cells was larger than that of CPT. The in vivo antitumour activity of all polymers in Balb/C mice bearing the sarcoma 180 tumour cell line was greater than that of CPT at a dose of 100 mg kg−1. Copyright © 2003 Society of Chemical Industry
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Keywords: 5‐norbonene‐endo‐2,3‐dicarboxylimidoundecanoyl camptothecin (NDUCPT); in vitro cytotoxicity; in vivo antitumour activity; photopolymerization; poly(NDUCPT‐co‐AA)

Document Type: Research Article

Affiliations: 1: Department of Premedical Sciences, College of Medicine, Kosin University, Pusan 602-703, Korea 2: Department of Polymer Science and Engineering, Pusan National University, Pusan 609-735, Korea 3: Department of Biochemistry, College of Medicine, Pusan National University, Pusan 609-735, Korea 4: Department of Chemistry, Pusan National University, Pusan 609-735, Korea 5: Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093-0358, USA

Publication date: August 1, 2003

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