| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 601112 | Colloids and Surfaces B: Biointerfaces | 2011 | 8 Pages |
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 (pHe), 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.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Carboxyl-modified hyperbranched polyether was complexed with cisplatin. ► The complex showed pH-responsive behavior. ► The pH-targeting of complex to tumor tissue exhibited an efficient anticancer effect.
