Varga Norbert, Bélteki Rita, Juhász Ádám, Csapó Edit
MTA-SZTE Lendület "Momentum" Noble Metal Nanostructures Research Group, University of Szeged, Rerrich B. Sqr. 1, H-6720 Szeged, Hungary.
Interdisciplinary Excellence Center, Department of Physical Chemistry and Materials Science, University of Szeged, Rerrich B. Sqr. 1, H-6720 Szeged, Hungary.
Pharmaceutics. 2023 Apr 28;15(5):1355. doi: 10.3390/pharmaceutics15051355.
The non-steroid anti-inflammatory drug ketoprofen (KP) as a model molecule is encapsulated in different poly(lactide-co-glycolide) (PLGA) nanostructured particles, using Tween20 (TWEEN) and Pluronic F127 (PLUR) as stabilizers to demonstrate the design of a biocompatible colloidal carrier particles with highly controllable drug release feature. Based on TEM images the formation of well-defined core-shell structure is highly favorable using nanoprecipitation method. Stabile polymer-based colloids with ~200-210 nm hydrodynamic diameter can be formed by successful optimization of the KP concentration with the right choice of stabilizer. Encapsulation efficiency (EE%) of 14-18% can be achieved. We clearly confirmed that the molecular weight of the stabilizer thus its structure greatly controls the drug release from the PLGA carrier particles. It can be determined that ~20% and ~70% retention is available with the use of PLUR and TWEEN, respectively. This measurable difference can be explained by the fact that the non-ionic PLUR polymer provides a steric stabilization of the carrier particles in the form of a loose shell, while the adsorption of the non-ionic biocompatible TWEEN surfactant results in a more compact and well-ordered shell around the PLGA particles. In addition, the release property can be further tuned by decreasing the hydrophilicity of PLGA by changing the monomer ratio in the range of ~20-60% (PLUR) and 70-90% (TWEEN).
以非甾体抗炎药酮洛芬(KP)作为模型分子,将其包裹于不同的聚(丙交酯-共-乙交酯)(PLGA)纳米结构颗粒中,使用吐温20(TWEEN)和普朗尼克F127(PLUR)作为稳定剂,以展示具有高度可控药物释放特性的生物相容性胶体载体颗粒的设计。基于透射电子显微镜(TEM)图像,采用纳米沉淀法非常有利于形成明确的核壳结构。通过成功优化KP浓度并正确选择稳定剂,可以形成流体动力学直径约为200 - 210 nm的稳定聚合物基胶体。包封率(EE%)可达14 - 18%。我们明确证实,稳定剂的分子量及其结构极大地控制了药物从PLGA载体颗粒中的释放。可以确定,分别使用PLUR和TWEEN时,药物保留率约为20%和70%。这种可测量的差异可以解释为,非离子型PLUR聚合物以松散壳的形式为载体颗粒提供空间稳定作用,而非离子型生物相容性吐温表面活性剂的吸附则在PLGA颗粒周围形成更紧密且有序的壳。此外,通过在约20 - 60%(PLUR)和70 - 90%(TWEEN)范围内改变单体比例来降低PLGA的亲水性,可进一步调节释放特性。