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MRI-visible and pH-sensitive micelles loaded with doxorubicin for hepatoma treatment


The emerging pH-sensitive polymeric nanocarriers carrying therapeutic drugs are bringing about new opportunities for effective treatment of cancer. A big challenge is to develop ultra pH-sensitive polymers, which is hard to achieve via introducing only one kind of pH-sensitive chemical structure with a specific pKa. In this study, an amphiphilic block copolymer, poly(ethylene glycol)-b-poly(β-benzyl L-aspartate) (mPEG-PBLA), was synthesized, and its PBLA block was aminolyzed by N,N-diisopropylamino ethylamine (DIP) and N,N-dibutalamino ethylamine (DBA) at different molar ratios. The copolymer mPEG-PAsp(DBA75%&DIP%) (PPAP75%) with an appropriate pKa was screened out to form pH-sensitive micelle which can encapsulate high content of hydrophobic anticancer drug doxorubicin (DOX) and magnetic resonance imaging (MRI) contrast agent superparamagnetic iron oxide nanoparticles (SPIONs) at neutral pH but disassemble rapidly under weak acidic conditions. The micellar nanodrug was efficiently taken up by HepG2 cells, and an intracellular DOX release was readily triggered inside acidic lysosomal compartments to allow migration of free drug to cell nucleus. The in vivo fluorescence and MR bimodal imaging showed that the pegylated nanodrug with suitable size and weak positive charge could stay longer in blood circulation and extravasate preferentially into tumor. The nanodrug not only exhibited high cytotoxicity in HepG2 cells but also significantly prolonged the survival time of tumor-bearing mice, demonstrating the great potential of pH-ultrasensitive and MRI-visible micelle for effective treatment of cancer.

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Publication details

The article was received on 18 Nov 2018, accepted on 03 Jan 2019 and first published on 09 Jan 2019

Article type: Paper
DOI: 10.1039/C8BM01501E
Citation: Biomater. Sci., 2019, Accepted Manuscript
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    MRI-visible and pH-sensitive micelles loaded with doxorubicin for hepatoma treatment

    B. Li, M. Cai, L. Lin, W. Sun, Z. Zhou, S. Wang, Y. Wang, K. Zhu and X. Shuai, Biomater. Sci., 2019, Accepted Manuscript , DOI: 10.1039/C8BM01501E

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