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Controlled co-delivery of hydrophilic and hydrophobic drugs from thermosensitive and crystallizable copolymer nanoparticles

机译:从热敏和可结晶的共聚物纳米颗粒中亲水和疏水药物的受控共输送

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Functionalized amphiphilic block copolymers poly(N-isopropyl acrylamide)-b-poly(stearyl methacrylate) (PNIPAM-PSMA) are synthesized. Their self-assembled core-shell nanoparticles have the hydrophilic thermosensitive shell and hydrophobic crystallizable core. Nanoparticles exhibit volume phase transition at temperature of 38 degrees C and its poly(stearyl methacrylate) (PSMA) moiety could form nano size crystals to retain drugs, making them good carriers for drug co-delivery system. Thermosensitivity and crystallinity of nanoparticles are characterized with dynamic light scattering (DLS), differential scanning calorimetry (DSC), small-angle X-ray scattering (SAXS), and atomic force microscopy (AFM). The interactions and relationship between chemical structures of copolymer nanoparticles and loading drugs are discussed. Different loading techniques and combined loading of hydrophobic/hydrophilic drugs are studied. Nanoparticles show a good and controllable drug loading capacity (DL) of hydrophilic/hydrophobic drugs. The drugs release kinetics is analyzed with Fick's law and Weibull model. A general method for analyzing drug release kinetics from nanoparticles is proposed. Weibull model is well fitted and the parameters with definite physical meaning are analyzed. PNIPAM-PSMA nanoparticles show a quite different thermal response, temporal regulation, and sustained release effect of hydrophilic and hydrophobic drugs, suggesting a promising application in extended and controlled co-delivery system of multi-drug. (c) 2016 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016, 133, 44132.
机译:合成了功能化的两亲嵌段共聚物聚(N-异丙基丙烯酰胺)-b-聚(甲基丙烯酸硬脂酯)(PNIPAM-PSMA)。它们的自组装核壳纳米粒子具有亲水性热敏壳和疏水性可结晶核。纳米粒子在38摄氏度的温度下表现出体积相变,其聚甲基丙烯酸硬脂基酯(PSMA)部分可形成纳米级晶体来保留药物,使其成为药物共递送系统的良好载体。纳米粒子的热敏性和结晶度通过动态光散射(DLS),差示扫描量热法(DSC),小角X射线散射(SAXS)和原子力显微镜(AFM)进行表征。讨论了共聚物纳米颗粒化学结构与载药的相互作用及相互关系。研究了疏水/亲水药物的不同装载技术和联合装载。纳米颗粒显示出良好的和可控制的亲水/疏水药物的载药量(DL)。用菲克定律和威布尔模型分析药物的释放动力学。提出了一种分析纳米颗粒药物释放动力学的通用方法。很好地拟合了威布尔模型,并分析了具有确定物理意义的参数。 PNIPAM-PSMA纳米颗粒表现出截然不同的热响应,时间调节以及亲水性和疏水性药物的持续释放效果,这表明在多药物的扩展和可控共递送系统中有希望的应用。 (c)2016 Wiley Periodicals,Inc. J. Appl。 Polym。科学2016,133,44132。

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