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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
A tumor pH-responsive complex: carboxyl-modified hyperbranched polyether and cis-dichlorodiammineplatinum(II)
Yumin Xia1, Yimin Wang, Yanping Wang
1College 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.
Colloids and Surfaces. B, Biointerfaces
|August 30, 2011
Summary
A novel polymer-platinum(II) complex (Suc-HPMHO-CDDP) demonstrates pH-targeting drug delivery for cancer therapy. This pH-responsive system effectively targets tumor tissues, enhancing cisplatin
Area of Science:
- Polymer Chemistry
- Nanomedicine
- Cancer Therapy
Background:
- Developing targeted drug delivery systems is crucial for improving cancer treatment efficacy.
- Tumor microenvironments exhibit acidic pH, presenting an opportunity for pH-responsive drug delivery.
Purpose of the Study:
- To design and prepare a pH-responsive polymer-platinum(II) complex for targeted delivery of cisplatin (CDDP).
- To evaluate the pH-targeting capability and antitumor efficacy of the developed complex.
Main Methods:
- Synthesis of carboxyl-modified hyperbranched polyether (Suc-HPMHO).
- Complexation of Suc-HPMHO with cisplatin (CDDP).
- Assessment of pH-responsiveness, cytotoxicity (MTT assay), and antitumor effects.
Main Results:
- Suc-HPMHO-CDDP exhibited reversible pH-response, with adjustable pH sensitivity.
- The complex showed low cytotoxicity and comparable antitumor efficacy to free CDDP.
- Suc-HPMHO-CDDP demonstrated pH-dependent deposition in acidic tumor environments, enabling pH-targeting.
Conclusions:
- The developed Suc-HPMHO-CDDP complex is a promising pH-targeting drug delivery system for cancer therapy.
- This approach offers enhanced drug accumulation at tumor sites due to the acidic tumor pH.

