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Novel thermo-sensitive core-shell nanoparticles for targeted paclitaxel delivery

机译：用于紫杉醇靶向靶向的新型热敏核壳纳米粒子

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Novel thermo-sensitive nanoparticles self-assembled from poly(N, N-diethylacrylamide-co-acrylamide)-block-poly(gamma-benzyl L-glutamate) were designed for targeted drug delivery in localized hyperthermia. The lower critical solution temperature (LCST) of nanoparticles was adjusted to a level between physiological body temperature (37 degrees C) and that used in local hyperthermia (about 43 degrees C). The temperature-dependent performances of the core-shell nanoparticles were systemically studied by nuclear magnetic resonance (NMR), circular dichroism (CD), fluorescence spectroscopy, dynamic light scattering (DLS), and atom force microscopy (AFM). The mean diameter of the nanoparticles increased slightly from 110 to 129 nm when paclitaxel (PTX), a poorly water-soluble anti-tumor drug, was encapsulated. A stability study in bovine serum albumin (BSA) solution indicated that the PTX loaded nanoparticles may have a long circulation time under physiological environments as the LCST was above physiological body temperature and the shell remained hydrophilic at 37 degrees C. The PTX release profiles showed thermo-sensitive controlled behavior. The proliferation inhibiting activity of PTX loaded nanoparticles was evaluated against Hela cells in vitro, compared with Taxol (a formulation of paclitaxel dissolved in Cremophor EL and ethanol). The cytotoxicity of PTX loaded nanoparticles increased obviously when hyperthermia was performed. The nanoparticles synthesized here could be an ideal candidate for thermal triggered anti-tumor PTX delivery system.
机译：从聚（N，N-二乙基丙烯酰胺-共-丙烯酰胺）-嵌段-聚（γ-苄基L-谷氨酸）自组装的新型热敏纳米粒子被设计用于局部热疗中的靶向药物递送。将纳米颗粒的较低临界溶液温度（LCST）调节至生理体温（37摄氏度）和局部热疗所用的较低临界溶液温度（约43摄氏度）之间的水平。通过核磁共振（NMR），圆二色性（CD），荧光光谱，动态光散射（DLS）和原子力显微镜（AFM）系统研究了核-壳纳米粒子的温度依赖性性能。当紫杉醇（PTX）（一种水溶性差的抗肿瘤药物）被封装时，纳米颗粒的平均直径从110 nm略微增加到129 nm。在牛血清白蛋白（BSA）溶液中的稳定性研究表明，当LCST高于生理体温且壳在37摄氏度下保持亲水性时，载有PTX的纳米颗粒在生理环境下可能具有较长的循环时间。敏感的受控行为。与紫杉醇（溶解在Cremophor EL和乙醇中的紫杉醇制剂）相比，在体外评估了负载PTX的纳米颗粒对Hela细胞的增殖抑制活性。进行高温治疗时，载有PTX的纳米颗粒的细胞毒性明显增加。此处合成的纳米粒子可能是热触发抗肿瘤PTX递送系统的理想候选者。

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