Theranostic pH-sensitive nanoparticles for highly efficient targeted delivery of doxorubicin for breast tumor treatment

作者：Changqie Pan, Yuqing Liu, Minyu Zhou, Wensheng Wang, Min Shi, Malcolm Xing, Wangjun Liao · 发表于：International Journal of Nanomedicine · 年份：2018 · DOI：10.2147/ijn.s147464 · 被引用次数：66 · 研究领域：Nanoparticle-Based Drug Delivery、Lanthanide and Transition Metal Complexes、Chemotherapy-induced cardiotoxicity and mitigation

Abstract: A multifunctional theranostic nanoplatform integrated with environmental responses has been developed rapidly over the past few years as a novel treatment strategy for several solid tumors. We synthesized pH-sensitive poly(β-thiopropionate) nanoparticles with a supermagnetic core and folic acid (FA) conjugation (FA-doxorubicin-iron oxide nanoparticles [ [email protected] ]) to deliver an antineoplastic drug, DOX, for the treatment of folate receptor (FR)-overexpressed breast cancer. In addition to an imaging function, the nanoparticles can release their payloads in response to an environment of pH 5, such as the acidic environment found in tumors. After chemical ( 1 H nuclear magnetic resonance) and physical (morphology and supermagnetic) characterization, [email protected] were shown to demonstrate pH-dependent drug release profiles. Western blotting analysis revealed the expression of FRs in three breast cancer cell lines, MCF-7, BT549, and MD-MBA-231. The cell counting kit-8 assay and transmission electron microscopy showed that [email protected] had the strongest cytotoxicity against breast cancer cells, compared with free DOX and non-FR targeted nanoparticles ( [email protected] ), and caused cellular apoptosis. The [email protected] cellular uptake and intracellular internalization were clarified by fluorescence microscopy. [email protected] plus magnetic field treatment suppressed in vivo tumor growth in mice to a greater extent than either treatment alone; f...