Poly(γ,l-glutamic acid)–cisplatin conjugate effectively inhibits human breast tumor xenografted in nude mice

摘要: An easily administered cis-dichlorodiammineplatinum (II) (CDDP) formulation with less toxicity and greater antitumor effect would be extremely valuable. We describe PGA-CDDP, a water-soluble CDDP derivative. The hydrolyzed gamma-PGA has molecular weight between 45 60 kDa, is water-soluble, biodegradable, nontoxic polymer produced by microbial fermentation. can released from the resulting conjugate in PBS: there was initially burst release during first 6h, followed sustained release. In vitro, PGA-CDDP potent than free at inhibiting cell growth Bcap-37 line. given as 3 doses an equivalent dose of 4 or 12 mg/kg 2-day intervals injections to Bcap-37-grafted mice. This treatment showed stronger activity toxic vivo. Antitumor assays demonstrated that had significantly higher control PBS (P 0.05 respect treatment), whereas same caused body loss 20-30% (P<0.001). These findings suggest PGA fermentation may used effective drug carrier for have potential applications human breast cancer.