Abstract：
Spherical gold/polyacrylic acid (Au/PAA) polymer-inorganic Janus nanoparticles (JNPs) with simultaneous therapeutic and targeting functions were fabricated. The obtained Au/PAA JNPs were further selectively functionalized with folic acid (FA) and thiol PEG amine (SH-PEG-NH2) on Au sides to provide superior biocompatibility and active targeting, while the other PAA sides were loaded with 5-aminolevulinic acid (5-ALA) to serve as a photosensitizer (PS) for photodynamic therapeutic (PDT) effects on MCF-7 cancer cells. The PS loading of 5-ALA was found to be 83% with an average hydrodynamic size and z-potential of 146 ± 0.8 nm and -6.40 mV respectively for FA-Au/PAA-ALA JNPs. The in vitro PDT study of the JNPs on MCF-7 breast cancer cells under 636 nm laser irradiation indicated the cell viability of 24.7% ± 0.5 for FA-Au/PAA-ALA JNPs at the IC50 value of 0.125 mM. In this regard, the actively targeted FA-Au/PAA-ALA JNPs treatment holds great potential for tumour therapy with high cancer cell-killing efficacy.
摘要：
制备了具有同时治疗和靶向功能的球形金/聚丙烯酸（Au/PAA）聚合物-无机Janus纳米颗粒（JNPs）。获得的Au/PAAJNPs在Au侧进一步用叶酸（FA）和巯基PEG胺（SH-PEG-NH2）选择性官能化，以提供优越的生物相容性和活性靶向性，而其他PAA侧负载有5-氨基乙酰丙酸（5-ALA）作为光敏剂（PS），用于对MCF-7癌细胞的光动力治疗（PDT）作用。对于FA-Au/PAA-ALAJNP，发现5-ALA的PS负载为83％，平均流体动力学尺寸和z电位分别为146±0.8nm和-6.40mV。在636nm激光照射下MCF-7乳腺癌细胞上JNP的体外PDT研究表明，FA-Au/PAA-ALAJNP的细胞活力为24.7%±0.5，IC50值为0.125mM。在这方面,主动靶向的FA-Au/PAA-ALAJNPs治疗在肿瘤治疗中具有巨大的潜力,具有高的癌细胞杀伤效力.
