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首页> 外文期刊>Journal of the American Chemical Society >Dimeric Drug Polymeric Nanoparticles with Exceptionally High Drug Loading and Quantitative Loading Efficiency
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Dimeric Drug Polymeric Nanoparticles with Exceptionally High Drug Loading and Quantitative Loading Efficiency

机译：具有超高载药量和定量载药效率的二聚药物聚合物纳米颗粒

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摘要

Encapsulation of small-molecule drugs in hydrophobic polymers or amphiphilic copolymers has been extensively used for preparing polymeric nanoparticles (NPs). The loadings and loading efficiencies of a wide range of drugs in polymeric NPs, however, tend to be very low. In this Communication, we report a strategy to prepare polymeric NPs with exceptionally high drug loading (＞50%) and quantitative loading efficiency. Specifically, a dimeric drug conjugate bearing a trigger-responsive domain was designed and used as the core-constructing unit of the NPs. Upon co-precipitation of the dimeric drug and methoxypoly(ethylene glycol)-block-polylactide (mPEG-PLA), NPs with a dimeric drug core and a polymer shell were formed. The high-drug-loading NPs showed excellent stability in physiological conditions. No premature drug or prodrug release was observed in PBS solution without triggering, while external triggering led to controlled release of drug in its authentic form.
机译：小分子药物在疏水性聚合物或两亲共聚物中的封装已被广泛用于制备聚合物纳米颗粒（NP）。但是，聚合物NP中多种药物的负载和负载效率往往非常低。在本通报中，我们报告了一种制备具有超高载药量（> 50％）和定量载药效率的聚合物NP的策略。具体而言，设计了带有触发反应域的二聚体药物缀合物，并将其用作NP的核心构建单元。在二聚体药物和甲氧基聚（乙二醇）-嵌段-聚丙交酯（mPEG-PLA）共同沉淀后，形成具有二聚体药物核心和聚合物壳的NP。高载药NP在生理条件下显示出极好的稳定性。在未触发的情况下，在PBS溶液中未观察到过早的药物释放或前药释放，而外部触发导致药物以其真实形式受控释放。

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  • 来源
    《Journal of the American Chemical Society》 |2015年第10期|3458-3461|共4页
  • 作者

    Kaimin Cai; Xi He; Ziyuan Song; Qian Yin; Yanfeng Zhang; Fatih M. Uckun; Chen Jiang; Jianjun Cheng;

  • 作者单位

    Department of Materials Science and Engineering, University of Illinois at Urbana-Champaign, Urbana, Illinois 61801, United States;

    Department of Materials Science and Engineering, University of Illinois at Urbana-Champaign, Urbana, Illinois 61801, United States,Key Laboratory of Smart Drug Delivery, Ministry of Education, Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai 201203, China;

    Department of Materials Science and Engineering, University of Illinois at Urbana-Champaign, Urbana, Illinois 61801, United States;

    Department of Materials Science and Engineering, University of Illinois at Urbana-Champaign, Urbana, Illinois 61801, United States;

    Department of Materials Science and Engineering, University of Illinois at Urbana-Champaign, Urbana, Illinois 61801, United States;

    Division of Hematology-Oncology, Systems Immunobiology Laboratory, Children's Center for Cancer and Blood Diseases, Children's Hospital Los Angeles, Los Angeles, California 90027, United States,Department of Pediatrics and Norris Comprehensive Cancer Center, University of Southern California, Keck School of Medicine, Los Angeles, California 90027, United States;

    Key Laboratory of Smart Drug Delivery, Ministry of Education, Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai 201203, China;

    Department of Materials Science and Engineering, University of Illinois at Urbana-Champaign, Urbana, Illinois 61801, United States;

  • 收录信息 美国《科学引文索引》(SCI);美国《工程索引》(EI);美国《生物学医学文摘》(MEDLINE);美国《化学文摘》(CA);
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