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生物相容性聚环氧乙烷-聚己内酯纳米胶束作为药物载体：结构与药物-聚合物相互作用

Biocompatible PEO-b-PCL Nanosized Micelles as Drug Carriers: Structure and Drug-Polymer Interactions.

作者信息

Chroni Angeliki, Mavromoustakos Thomas, Pispas Stergios

机构信息

Theoretical and Physical Chemistry Institute, National Hellenic Research Foundation, 48 Vassileos Constantinou Avenue, 11635 Athens, Greece.

Department of Chemistry, National and Kapodistrian University of Athens, Panepistimioupolis, 15771 Zografou, Greece.

出版信息

Nanomaterials (Basel). 2020 Sep 18;10(9):1872. doi: 10.3390/nano10091872.

DOI:10.3390/nano10091872
PMID:32962043
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7559820/
Abstract

We report on the preparation of drug nanocarriers by encapsulating losartan potassium (LSR) into amphiphilic block copolymer micelles, utilizing the biocompatible/biodegradable poly(ethylene oxide)-b-poly(ε-caprolactone) (PEO-b-PCL) diblock copolymer. The PEO-b-PCL micelles and LSR-loaded PEO-b-PCL nanocarriers were prepared by organic solvent evaporation method (OSEM). Light scattering and nuclear magnetic resonance (NMR) provide information on micelle structure and polymer-drug interactions. According to dynamic light scattering (DLS) analysis, the PEO-b-PCL micelles and LSR-loaded PEO-b-PCL nanocarriers formed nanostructures in the range of 17-26 nm in aqueous milieu. Attenuated total reflection Fourier transform infrared (ATR-FTIR) and ultraviolet-visible (UV-Vis) measurements confirmed the presence of LSR in the polymeric drug solutions. NMR results proved the successful encapsulation of LSR into the PEO-b-PCL micelles by analyzing the drug-micelles intermolecular interactions. Specifically, 2D-NOESY experiments clearly evidenced the intermolecular interactions between the biphenyl ring and butyl chain of LSR structure with the methylene signals of PCL. Additionally, NMR studies as a function of temperature demonstrated an unexpected, enhanced proton mobility of the PEO-b-PCL micellar core in DO solutions, probably caused by the melting of the PCL hydrophobic core.

摘要

我们报道了通过将氯沙坦钾（LSR）包裹于两亲性嵌段共聚物胶束中来制备药物纳米载体，所使用的是具有生物相容性/可生物降解性的聚（环氧乙烷）-b-聚（ε-己内酯）（PEO-b-PCL）二嵌段共聚物。PEO-b-PCL胶束和负载LSR的PEO-b-PCL纳米载体通过有机溶剂蒸发法（OSEM）制备。光散射和核磁共振（NMR）提供了关于胶束结构和聚合物-药物相互作用的信息。根据动态光散射（DLS）分析，PEO-b-PCL胶束和负载LSR的PEO-b-PCL纳米载体在水性介质中形成了17 - 26 nm范围内的纳米结构。衰减全反射傅里叶变换红外光谱（ATR-FTIR）和紫外-可见光谱（UV-Vis）测量证实了聚合物药物溶液中存在LSR。NMR结果通过分析药物-胶束分子间相互作用证明了LSR成功包裹于PEO-b-PCL胶束中。具体而言，二维核Overhauser效应光谱（2D-NOESY）实验清楚地证明了LSR结构的联苯环和丁基链与PCL的亚甲基信号之间的分子间相互作用。此外，作为温度函数的NMR研究表明，在氘代甲醇（DO）溶液中PEO-b-PCL胶束核心的质子迁移率意外增强，这可能是由PCL疏水核心的熔化引起的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/b6842e159b50/nanomaterials-10-01872-g012.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/612a59342d5e/nanomaterials-10-01872-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/b36744924466/nanomaterials-10-01872-g006.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/280bfe7a9dd8/nanomaterials-10-01872-g008.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/65b5e71b5452/nanomaterials-10-01872-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/b6842e159b50/nanomaterials-10-01872-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/ef26ca1393a4/nanomaterials-10-01872-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/f9cb33ce477f/nanomaterials-10-01872-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/b93686467f45/nanomaterials-10-01872-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/accf862e548a/nanomaterials-10-01872-g003.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/612a59342d5e/nanomaterials-10-01872-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/b36744924466/nanomaterials-10-01872-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/141139438df0/nanomaterials-10-01872-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/280bfe7a9dd8/nanomaterials-10-01872-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/c8a6cdb76044/nanomaterials-10-01872-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/3a1375c59f45/nanomaterials-10-01872-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/65b5e71b5452/nanomaterials-10-01872-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2638/7559820/b6842e159b50/nanomaterials-10-01872-g012.jpg

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