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Molecular Insight into Drug-Loading Capacity of PEG–PLGA Nanoparticles for Itraconazole
The Journal of Physical Chemistry B ( IF 3.3 ) Pub Date : 2018-07-05 , DOI: 10.1021/acs.jpcb.8b03742 Natalia Wilkosz 1 , Grzegorz Łazarski 1 , Lubomir Kovacik 2 , Patrycja Gargas 1 , Maria Nowakowska 1 , Dorota Jamróz 1 , Mariusz Kepczynski 1
The Journal of Physical Chemistry B ( IF 3.3 ) Pub Date : 2018-07-05 , DOI: 10.1021/acs.jpcb.8b03742 Natalia Wilkosz 1 , Grzegorz Łazarski 1 , Lubomir Kovacik 2 , Patrycja Gargas 1 , Maria Nowakowska 1 , Dorota Jamróz 1 , Mariusz Kepczynski 1
Affiliation
Nanoparticles made of amphiphilic block copolymers comprising biodegradable core-forming blocks are very attractive for the preparation of drug-delivery systems with sustained release. Their therapeutic applications are, however, hindered by low values of the drug-loading content (DLC). The compatibility between the drug and the core-forming block of the copolymer is considered the most important factor affecting the DLC value. However, the molecular picture of the hydrophobic drug–copolymer interaction is still not fully recognized. Herein, we examined this complex issue using a range of experimental techniques in combination with atomistic molecular dynamics simulations. We performed an analysis of the interaction between itraconazole, a model hydrophobic drug, and a poly(ethylene glycol)–poly(lactide-co-glycolide) (PEG–PLGA) copolymer, a biodegradable copolymer commonly used for the preparation of drug-delivery systems. Our results clearly show that the limited capacity of the PEG–PLGA nanoparticles for the accumulation of hydrophobic drugs is due to the fact that the drug molecules are located only at the water–polymer interface, whereas the interior of the PLGA core remains empty. These findings can be useful in the rational design and development of amphiphilic copolymer-based drug-delivery systems.
中文翻译:
PEG-PLGA纳米颗粒对伊曲康唑载药量的分子洞察
由包含可生物降解的核形成嵌段的两亲嵌段共聚物制成的纳米颗粒对于制备具有持续释放的药物递送系统非常有吸引力。然而,它们的治疗应用由于低的载药量(DLC)而受到阻碍。药物与共聚物的核形成嵌段之间的相容性被认为是影响DLC值的最重要因素。然而,疏水性药物-共聚物相互作用的分子图仍然没有被完全认识到。在这里,我们使用一系列实验技术结合原子分子动力学模拟研究了这个复杂的问题。我们-聚执行伊曲康唑之间的相互作用的分析,模型疏水性药物,和聚(乙二醇)(丙交酯-共-乙交酯(PEG-PLGA)共聚物,一种可生物降解的共聚物,通常用于制备药物递送系统。我们的结果清楚地表明,PEG-PLGA纳米颗粒对疏水性药物积累的能力有限是由于以下事实:药物分子仅位于水-聚合物界面,而PLGA核心的内部仍然是空的。这些发现可用于合理设计和开发基于两亲共聚物的药物递送系统。
更新日期:2018-07-08
中文翻译:
PEG-PLGA纳米颗粒对伊曲康唑载药量的分子洞察
由包含可生物降解的核形成嵌段的两亲嵌段共聚物制成的纳米颗粒对于制备具有持续释放的药物递送系统非常有吸引力。然而,它们的治疗应用由于低的载药量(DLC)而受到阻碍。药物与共聚物的核形成嵌段之间的相容性被认为是影响DLC值的最重要因素。然而,疏水性药物-共聚物相互作用的分子图仍然没有被完全认识到。在这里,我们使用一系列实验技术结合原子分子动力学模拟研究了这个复杂的问题。我们-聚执行伊曲康唑之间的相互作用的分析,模型疏水性药物,和聚(乙二醇)(丙交酯-共-乙交酯(PEG-PLGA)共聚物,一种可生物降解的共聚物,通常用于制备药物递送系统。我们的结果清楚地表明,PEG-PLGA纳米颗粒对疏水性药物积累的能力有限是由于以下事实:药物分子仅位于水-聚合物界面,而PLGA核心的内部仍然是空的。这些发现可用于合理设计和开发基于两亲共聚物的药物递送系统。