用于磁性靶向治疗肺纤维化的聚多巴胺包覆的Fe3O4/甲强龙/环磷酰胺复合超粒子

肺纤维化是一种致命性肺部疾病, 目前临床常规的甲强龙(MPS)联合环磷酰胺(CTX)治疗方法存在明显的不良反应. 基于降低药物毒副作用的目的, 本文设计了一种聚多巴胺(PDA)包覆的Fe₃O₄纳米粒子/甲强龙/环磷酰胺复合超粒子(Fe₃O₄/MPS/CTX@PDA SPs), 提出磁性靶向治疗肺纤维化的思路. 从预制的油溶性Fe₃O₄纳米粒子出发, 通过水包油微乳液模板法制备了Fe₃O₄ 超粒子(SPs), 并在进一步包覆PDA壳层的过程中引入MPS和CTX, 制备了Fe₃O₄/MPS/CTX@PDA SPs, 考察了Fe₃O₄/MPS/CTX@PDA SPs的稳定性、 磁性、 对MPS和CTX的负载及释放, 分析了其生物毒性, 并建立动物模型验证了其磁性靶向功能.     

Superparticles Formed by Amphiphilic Tadpole-like Single Chain Polymeric Nanoparticles and Their Application as an Ultrasonic Responsive Drug Carrier

Herein, we report self-assembly of tadpole-like single chain polymeric nanoparticles (TPPs) and the ultrasonic response of the resultant superparticles. The TPPs are with an intramolecularly crosslinked poly(2-(methacryloyloxy)ethyl pent-4-ynoate)-r-poly(hydroxyethyl methacrylate) (PMAEP-r-PHEMA) chain as the "head" and a poly(2-(dimethylamino)ethyl methacrylate (PDMAEMA) linear chain as the "tail", and are pre-pared simply and efficiently by Glaser-coupling of the pendant alkynes in the PMAEP-r-PHEMA block in the common solvent methanol. The formation of the TPPs was confirmed by gel permeation chromatograph, nuclear magnetic resonance spectroscopy, dynamic light scattering, static dynamic scattering, and transmission electron microscopy. In aqueous solution, the amphiphilic TPPs could self-assemble into regular superparticles, driven by ag-gregation of the hydrophobic "heads". Since in the structure there is no chain entanglement and the embedding of PDMAEMA chains disturb close-packing of the "heads", the superpar-ticles are responsive to a low-energy ultrasonic vibration, as evidenced by greatly enhanced release of the functional molecules from the superparticles by treatment of a low-energy ultrasound. Therefore, the superparticles should be very promising in the use as the drug carriers that can be manipulated from a long distance, considering that ultrasonic energy can be focused at a small area in a relatively long distance from the ultrasound-radiating source.     

两亲性单链蝌蚪状聚合物纳米粒子组装形成超级粒子及其超声响应性研究

Herein, we report self-assembly of tadpole-like single chain polymeric nanoparticles (TPPs) and the ultrasonic response of the resultant superparticles. The TPPs are with an intramolecularly crosslinked poly(2-(methacryloyloxy)ethyl pent-4-ynoate)-r-poly(hydroxyethyl methacrylate) (PMAEP-r-PHEMA) chain as the "head" and a poly(2-(dimethylamino)ethyl methacrylate (PDMAEMA) linear chain as the "tail", and are pre-pared simply and efficiently by Glaser-coupling of the pendant alkynes in the PMAEP-r-PHEMA block in the common solvent methanol. The formation of the TPPs was confirmed by gel permeation chromatograph, nuclear magnetic resonance spectroscopy, dynamic light scattering, static dynamic scattering, and transmission electron microscopy. In aqueous solution, the amphiphilic TPPs could self-assemble into regular superparticles, driven by ag-gregation of the hydrophobic "heads". Since in the structure there is no chain entanglement and the embedding of PDMAEMA chains disturb close-packing of the "heads", the superpar-ticles are responsive to a low-energy ultrasonic vibration, as evidenced by greatly enhanced release of the functional molecules from the superparticles by treatment of a low-energy ultrasound. Therefore, the superparticles should be very promising in the use as the drug carriers that can be manipulated from a long distance, considering that ultrasonic energy can be focused at a small area in a relatively long distance from the ultrasound-radiating source.