title: A tumor pH-responsive complex: carboxyl-modified hyperbranched polyether and cis-dichlorodiammineplatinum(II).
abstract: To realize the pH-targeting delivery of antitumor drug cis-dichlorodiammineplatinum(II) (cisplatin, CDDP), a tumor pH-responsive polymer-platinum(II) complex (Suc-HPMHO-CDDP) from carboxyl-modified hyperbranched polyether (Suc-HPMHO) and cisplatin was designed and prepared. Because of the existence of hydrophobic core and ionization of surface carboxylic acid, Suc-HPMHO showed reversible pH-response in aqueous solution, and its responding pH value could be readily adjusted by only changing the degree of carboxylation of Suc-HPMHO. With plenty of terminal carboxyl groups, Suc-HPMHO could form the complex with CDDP by substituting the chloride ions with carboxyls. Methyl tetrazolium (MTT) assay showed that Suc-HPMHO had low cytotoxicity, while Suc-HPMHO-CDDP complex presented a similar antitumor effect with the free CDDP. Under the tumor acidic pH (pH(e)), Suc-HPMHO-CDDP complex deposited around/in cells because of its pH-response. Therefore, the pH-targeting of Suc-HPMHO-CDDP complex to tumor tissue could be realized. All of these results show that the tumor pH-responsive Suc-HPMHO-CDDP complex is a potential pH-targeting drug delivery system in cancer therapy.
authors.affiliation: College of Materials Science and Engineering, State Key Laboratory for Modification of Chemical Fibers and Polymer Material, Donghua University, 2999 North Renmin Road, Shanghai 201620, People's Republic of China.
authors.forename: Yumin
authors.initials: Y
authors.lastname: Xia
authors.forename: Yimin
authors.initials: Y
authors.lastname: Wang
authors.forename: Yanping
authors.initials: Y
authors.lastname: Wang
authors.forename: Chunlai
authors.initials: C
authors.lastname: Tu
authors.forename: Feng
authors.initials: F
authors.lastname: Qiu
authors.forename: Lijuan
authors.initials: L
authors.lastname: Zhu
authors.forename: Yue
authors.initials: Y
authors.lastname: Su
authors.forename: Deyue
authors.initials: D
authors.lastname: Yan
authors.forename: Bangshang
authors.initials: B
authors.lastname: Zhu
authors.forename: Xinyuan
authors.initials: X
authors.lastname: Zhu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000737:chemistry*; D019556:COS Cells; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D002945:Cisplatin / Q000008:administration & dosage* / Q000737:chemistry*; D004337:Drug Carriers / Q000009:adverse effects / Q000737:chemistry; D016503:Drug Delivery Systems / Q000009:adverse effects / Q000379:methods; D006367:HeLa Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D011108:Polymers / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D011108:Polymers; D002945:Cisplatin