Journal
COLLOIDS AND SURFACES B-BIOINTERFACES
Volume 88, Issue 2, Pages 674-681Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.colsurfb.2011.07.059
Keywords
Hyperbranched polymer; Cisplatin; Drug delivery; pH-responsive
Funding
- National Natural Science Foundation of China [20974062]
- National Basic Research Program [2009CB930400]
- Shanghai Leading Academic Discipline Project [B603, B202]
- China National Funds for Distinguished Young Scientists [21025417]
- Donghua University
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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. (C) 2011 Elsevier B.V. All rights reserved.
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