Publication: Enhanced selective cytotoxicity of doxorubicin to breast cancer cells by methoxypolyethylene glycol conjugation via a novel beta-thiopropanamide linker
Issued Date
2020-12-05
Resource Type
ISSN
00143057
Other identifier(s)
2-s2.0-85092526437
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Mahidol University
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SCOPUS
Bibliographic Citation
European Polymer Journal. Vol.141, (2020)
Suggested Citation
Wiwat Supasena, Chawanphat Muangnoi, Kemika Praengam, Tin Wui Wong, Guanyinsheng Qiu, Shengqing Ye, Jie Wu, Somboon Tanasupawat, Pornchai Rojsitthisak Enhanced selective cytotoxicity of doxorubicin to breast cancer cells by methoxypolyethylene glycol conjugation via a novel beta-thiopropanamide linker. European Polymer Journal. Vol.141, (2020). doi:10.1016/j.eurpolymj.2020.110056 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/59927
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Title
Enhanced selective cytotoxicity of doxorubicin to breast cancer cells by methoxypolyethylene glycol conjugation via a novel beta-thiopropanamide linker
Abstract
© 2020 Elsevier Ltd Doxorubicin (DOX) is a chemotherapeutic agent that suffers from severe adverse effects due to non-selective cell cytotoxicity. This study designs a novel beta-thiopropanamide linker (A) which conjugates DOX with methoxypolyethylene glycol (mPEG) to sustain systemic drug release, and to promote cancer enzyme-responsiveness and cell selectivity. The mPEG-DOX conjugate with the beta-thiopropanamide linker (P-A-DOX) conjugate was synthesized using thiol-functionalized methoxypolyethylene glycol and acrylic acid to establish the beta-thiopropanamide linkage with DOX, with the mPEG-DOX (P-DOX) conjugate as the control. The conjugates were structurally characterized by NMR, chemical assay, transmission electron microscopy and dynamic light scattering technique. The in vitro hydrolytic stability as a function of pH and cytotoxicity tests (MDA-MB-231 and MCF-7 breast cancer cells vs MCF-10A noncancerous cells) were performed. The P-A-DOX and P-DOX conjugates can self-assemble into nanoparticles. The P-A-DOX and P-DOX conjugates exhibited sustained drug release and improved physicochemical stability under physiological pHs. Their cancer cell cytotoxicity and selectivity progressed in the following order: P-A-DOX > P-DOX > DOX. The P-A-DOX conjugate with the beta-thiopropanamide linker is a selective DOX nanodelivery system for breast cancer treatment.
