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首页> 美国卫生研究院文献>Scientia Pharmaceutica >Lectin-Grafted PLGA Microcarriers Loaded with Fluorescent Model Drugs: Characteristics Release Profiles and Cytoadhesion Studies
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Lectin-Grafted PLGA Microcarriers Loaded with Fluorescent Model Drugs: Characteristics Release Profiles and Cytoadhesion Studies

机译：载有荧光模型药物的凝集素接枝的PLGA微载体：特性释放曲线和细胞粘附研究

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PLGA microparticles loaded with three different fluorescent model drugs, fluorescein sodium (hydrophilic), sulforhodamine (amphoteric), and boron-dipyrromethene (BODIPY® 493/503, lipophilic), were prepared by the solvent evaporation technique. Due to varying hydrophilicity, the diameters of the microparticles ranged between 4.1 and 4.7 μm. According to fluorimetric analysis, the loading varied from 0.06 to 2.25 μg of the model drug per mg PLGA. In terms of the release profile, the fluorescein sodium-entrapped formulation exhibited thermo-responsive release kinetics. In the case of sulforhodamine- and BODIPY® 493/503-loaded particles, almost no release was observed, neither at 4°C nor 37°C during the first 50 hours. Furthermore, to estimate the bioadhesive properties of such drug delivery systems, the surface of the loaded particles was grafted with wheat germ agglutinin by applying the carbodiimide method. Cytoadhesion studies with Caco-2 monolayers revealed an up to 1.9-fold and 3.6-fold increase in the bioadhesion of the lectin-functionalized, model drug-loaded particles as compared to the albumin- and non-grafted microcarriers, respectively. All in all, the results clearly indicated that the lipophilicity of the polymer matching that of the drug favored entrapment, whereas mismatching impeded loading into the PLGA-microparticles. Even in the case of low loading, these delivery systems might be useful for the fluorescent detections and microscopic imaging of cellular interactions due to their fluorescent properties and lack of dye leakage. Moreover, lectin grafting can mediate bioadhesive properties to such particulate drug carriers which could be a promising approach to improve drug delivery.
机译：通过溶剂蒸发技术制备了载有三种不同荧光模型药物荧光素钠（亲水性），磺基罗丹明（两性）和硼二吡咯亚甲基（BODIPY s 493/503，亲脂性）的PLGA微粒。由于亲水性的变化，微粒的直径在4.1至4.7μm之间。根据荧光分析，每mg PLGA的载药量为0.06至2.25μg模型药物。就释放曲线而言，荧光素钠包裹的制剂表现出热响应释放动力学。对于装载有磺基若丹明和BODIPY ® 493/503的颗粒，在最初的50小时内，无论是在4°C还是在37°C，都几乎没有观察到释放。此外，为了估计这种药物递送系统的生物粘附特性，通过应用碳二亚胺方法将负载的颗粒表面嫁接到小麦胚芽凝集素上。用Caco-2单层进行的细胞粘附研究表明，与白蛋白微载体和非移植微载体相比，凝集素功能化的模型药物负载颗粒的生物粘附分别增加了1.9倍和3.6倍。总而言之，结果清楚地表明，聚合物的亲脂性与药物的亲脂性有利于包封，而错配则阻碍了向PLGA微粒中的负载。即使在低负荷的情况下，由于它们的荧光特性和缺乏染料渗漏，这些递送系统对于细胞相互作用的荧光检测和显微成像也可能有用。而且，凝集素接枝可以介导对这种颗粒状药物载体的生物粘附特性，这可能是改善药物输送的有前途的方法。

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