Expansile Nanoparticles: Synthesis, Characterization, and in Vivo Efficacy of an Acid-Responsive Polymeric Drug Delivery System
Expansile Nanoparticles: Synthesis, Characterization, and in Vivo Efficacy of an Acid-Responsive Polymeric Drug Delivery System
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DOI：
10.1021/ja807416t
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发表时间：
2009-02-25
影响因子：
15
通讯作者：
Grinstaff, Mark W.
中科院分区：
文献类型：
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作者：
Griset, Aaron P.;Walpole, Joseph;Grinstaff, Mark W.
纳米颗粒在药物递送应用中的用途越来越多，作为提高治疗效果和改善患者护理的手段。在这里，我们报告了工程聚合物纳米颗粒，在pH 5下经历疏水性到亲水性的转变，以提供溶胀和快速释放其内容物。由于我们的临床兴趣与预防切除术后肺肿瘤复发有关，因此在模拟微观疾病的模型中评估了纳米颗粒，类似于手术后可能保留在切除边缘的残留隐匿性肿瘤。紫杉醇是一种难溶于水的抗癌药物，可膨胀的纳米颗粒装载，防止建立在体内肺癌，是上级的紫杉醇的传统药物输送方法，使用Cremophor EL/乙醇。
Nanoparticles are finding increased uses in drug delivery applications as a means to increase treatment efficacy and improve patient care. Here, we report engineered polymeric nanoparticles that undergo a hydrophobic to hydrophilic transition at pH 5 to afford swelling and rapid release of their contents. As our clinical interest ties in the prevention of lung tumor recurrence following resection, the nanoparticles were evaluated in a model mimicking microscopic disease, akin to residual occult tumor that can remain at the resection margin following surgery. Expansile nanoparticles loaded with paclitaxel, a poorly water-soluble anticancer drug, prevent establishment of lung cancer in vivo and are superior to the conventional drug delivery method for paclitaxel using Cremophor EL/ethanol.