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Synthesis of core@shell nanoparticles functionalized with folic acid-modified PCL-co-PEGMA copolymer for methotrexate delivery
Nano-Structures & Nano-Objects Pub Date : 2021-02-12 , DOI: 10.1016/j.nanoso.2021.100675
João Victor Brandt , Rodolfo Debone Piazza , Caio Carvalho dos Santos , Jaime Vega-Chacón , Bruno Estevam Amantéa , Gabriel Cardoso Pinto , Miguel Jafelicci , Rodrigo Fernando Costa Marques

Cancer is responsible for many fatalities and it is considered a public health problem. The side effects caused by conventional treatment are aggressive and painful to patients and can be reduced using nanomaterials that allows action in specific sites, making the cancer treatment more efficient, improving patient life’s quality. Many kinds of nanoparticles that can be used, among these the block copolymer functionalized iron oxide nanoparticles stand out due to their simultaneous interaction with hydrophobic and hydrophilic drugs. The evaluation of these platforms properties allows optimizing their action in the human body, enhancing its biodistribution and targeting a specific region in the organism. The encapsulation efficiency and the controlled release profile is strictly dependent on the size, morphology, and interactions of the copolymer blocks. In this work, it was studied the synthesis of a hybrid nanoplatform composed of an inorganic core (iron oxide) and a polymeric shell (PCL-co-PEGMA block copolymer modified with folic acid). FTIR and 1H NMR allowed the confirmation of the nanoplatform synthesis. Particles around 180 nm stable at physiological pH were obtained, allowing its application in different regions of the human body. The encapsulation efficiency of methotrexate was approximately 95%. The drug delivery assays indicated that the nanoplatform is less active at pH 2; the presence of reduced glutathione enhanced the methotrexate release, reaching almost 50% methotrexate release after 96 h of analysis. The release efficiency of the nanoplatform allowed to identify its potential as a controlled drug delivery system.



中文翻译:

叶酸修饰的PCL-co-PEGMA共聚物功能化的甲壳素释放用功能的核壳纳米粒子的合成

癌症是造成许多死亡的原因,被认为是公共健康问题。常规治疗引起的副作用会给患者带来侵略性和痛苦,并且可以使用允许在特定部位起作用的纳米材料来减轻这种副作用,从而使癌症治疗更加有效,从而改善了患者的生活质量。由于嵌段共聚物官能化的氧化铁纳米颗粒与疏水性和亲水性药物同时相互作用,因此可以使用的纳米颗粒种类很多。对这些平台特性的评估可以优化它们在人体中的作用,增强其生物分布并靶向生物体中的特定区域。包封效率和控释曲线严格取决于尺寸,形态,和共聚物嵌段的相互作用。在这项工作中,研究了由无机核(氧化铁)和聚合物壳(用叶酸改性的PCL-co-PEGMA嵌段共聚物)组成的杂化纳米平台的合成。FTIR和1 H NMR证实了纳米平台合成。获得了在生理pH下稳定的约180 nm的颗粒,使其可应用于人体的不同区域。甲氨蝶呤的包封效率约为95%。药物传递测定表明,纳米平台在pH 2时活性较低。还原型谷胱甘肽的存在增强了甲氨蝶呤的释放,在分析96小时后达到了近50%的甲氨蝶呤释放。纳米平台的释放效率可以确定其作为受控药物输送系统的潜力。

更新日期:2021-02-12
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