Antitumor Efficacy of Colon-Specific HPMA Copolymer/9-Aminocamptothecin Conjugates in Mice Bearing Human-Colon Carcinoma Xenografts

作者：Gao Song Qi; Sun Yongen; Kopeckova Pavla; Peterson C Matthew; Kopecek Jindrich^*

来源：Macromolecular Bioscience, 2009, 9(11): 1135-1142.

DOI：10.1002/mabi.200900147

• antitumor efficacy
• colon-specific drug delivery
• HPMA-copolymer/9-aminocamptothecin conjugate
• human-colon carcinoma xenografts

The antitumor activity of a colon-specific N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer - 9-aminocamptothecin (9-AC) conjugate (P-9-AC) was assessed in orthotopic and subcutaneous animal (HT29 xenograft) tumor models. P-9-AC treatment of mice bearing orthotopic colon tumors, with a dose of 3 mg/kg of 9-AC equivalent every other day for 6 weeks, resulted in regression of tumors in 9 of 10 mice. A lower dose of P-9-AC (1.25 mg/kg of 9-AC equivalent) every other day for 8 weeks inhibited subcutaneous tumor growth in all mice. No liver metastases were observed. Colon-specific release of 9-AC from polymer conjugates enhanced antitumor activity and minimized the systemic toxicity.

• 出版日期2009-11-10