Kazsoki Adrienn, Szabó Péter, Süvegh Károly, Vörös Tamás, Zelkó Romána
University Pharmacy Department of Pharmacy Administration, Semmelweis University,Hőgyes Endre St. 7-9, H-1092 Budapest, Hungary.
Laboratory of Nuclear Chemistry, Eötvös Loránd University/HAS Chemical Research Center, P.O. Box 32, H-1518 Budapest, Hungary.
J Pharm Biomed Anal. 2017 Sep 5;143:62-67. doi: 10.1016/j.jpba.2017.05.035. Epub 2017 May 27.
Electrospun papaverine hydrochloride-loaded nanofibrous sheets consist of hydroxypropyl cellulose/poly(vinyl alcohol) composite were prepared for buccal administration for cerebral ischemia. The nanofibrous drug delivery system was subjected to accelerated stability test for four weeks in order to scrutinize the solid state changes relating to the stress induced (40±2°C/75±5% relative humidity) physical ageing. Micro- and macrostructural alterations were detected using scanning electron microscopy (SEM), Raman spectroscopy, Fourier transform infrared spectroscopy (FTIR) and positron annihilation lifetime spectroscopy (PALS). Significant changes were revealed at both supramolecular and macroscopic levels. Microscopic morphology uncovered major morphological transitions. Subtle variations of Raman and FTIR spectra indicated that the local chemical environment of papaverine was altered suggesting a partial phase transition of the active. Discrete o-Ps lifetimes and lifetime-distributions unveiled a two-step ageing process of the drug carrier. In addition to the tracking of the glassy-to-rubbery transition of the fiber forming polymers, the Raman spectroscopy enabled monitoring the kinetics of the phase transition observed.
制备了由羟丙基纤维素/聚乙烯醇复合材料组成的载盐酸罂粟碱的电纺纳米纤维片，用于脑缺血的口腔给药。对纳米纤维药物递送系统进行了为期四周的加速稳定性试验，以研究与应力诱导（40±2°C/75±5%相对湿度）物理老化相关的固态变化。使用扫描电子显微镜（SEM）、拉曼光谱、傅里叶变换红外光谱（FTIR）和正电子湮没寿命光谱（PALS）检测微观和宏观结构变化。在超分子和宏观水平上均发现了显著变化。微观形态揭示了主要的形态转变。拉曼光谱和FTIR光谱的细微变化表明罂粟碱的局部化学环境发生了改变，这表明活性成分发生了部分相变。离散的邻位正电子寿命和寿命分布揭示了药物载体的两步老化过程。除了跟踪成纤聚合物的玻璃态到橡胶态转变外，拉曼光谱还能够监测观察到的相变动力学。
