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Bortezomib-Catechol Conjugated Prodrug micelles: Combining Bone Targeting and Aryl Boronate-based pH-Responsive Drug Release for Cancer Bone-metastasis Therapy

Abstract

The treatment of metastatic tumor is highly undesirable in clinics, which also arouse great concerns in the design of nanoscale drug delivery system. Bone metastasis is one of the most common pathways in the metastasis of breast cancer, and it is also an important cause for the tumor recurrence and death. Aryl boronate group, as acidity-labile linker, has been introduced into nano-assembly in recent years. Especially, as a proteasome inhibitor anticancer drug with boric acid group, bortezomib could facilitate the formation of pH-sensitive aryl boric acid ester linkage with catecholic group. In this study, a bortezomib-loaded micelle with bone targeting properties was constructed for treatment of breast cancer bone metastasis. The mixed micelles employed alendronate (ALN) as bone-targeting ligand and encapsulated bortezomib-catechol conjugates as cargoes. In vitro and in vivo studies showed that, compared with free drugs or controlled micelles, this prodrug micelle (ALN-NP) exhibited many favorable properties, such as reducing systemic toxicity and improving therapeutic effect. Therefore, promising potentials are clearly shown by ALN-NP as nanovehicle for bone-targeting delivery of chemotherapeutic drugs. More attractively, this work offers a novel combination strategy of bone targeting and aryl boronate-based pH-responsive drug release for anti-metastasis therapy.

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Publication details

The article was received on 14 May 2018, accepted on 24 Aug 2018 and first published on 28 Aug 2018


Article type: Paper
DOI: 10.1039/C8NR03899F
Citation: Nanoscale, 2018, Accepted Manuscript
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    Bortezomib-Catechol Conjugated Prodrug micelles: Combining Bone Targeting and Aryl Boronate-based pH-Responsive Drug Release for Cancer Bone-metastasis Therapy

    J. Zhu, Q. Huo, M. Xu, F. Yang, Y. Li, H. Shi, Y. Niu and Y. Liu, Nanoscale, 2018, Accepted Manuscript , DOI: 10.1039/C8NR03899F

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