Sipos Emese, Kósa Nóra, Kazsoki Adrienn, Szabó Zoltán-István, Zelkó Romána
Department of Drugs Industry and Pharmaceutical Management, University of Medicine, Pharmacy, Sciences and Technology of Targu Mures, Gheorghe Marinescu 38, 540139 Targu Mures, Romania.
University Pharmacy Department of Pharmacy Administration, Semmelweis University, H-1092 Hőgyes Endre utca 7-9, 1092 Budapest, Hungary.
Pharmaceutics. 2019 Aug 17;11(8):417. doi: 10.3390/pharmaceutics11080417.
Aceclofenac-loaded poly(vinyl-pyrrolidone)-based nanofiber formulations were prepared by electrospinning to obtain drug-loaded orally disintegrating webs to enhance the solubility and dissolution rate of the poorly soluble anti-inflammatory active that belongs to the BCS Class-II. Triethanolamine-containing ternary composite of aceclofenac-poly(vinyl-pyrrolidone) nanofibers were formulated to exert the synergistic effect on the drug-dissolution improvement. The composition and the electrospinning parameters were changed to select the fibrous sample of optimum fiber characteristics. To determine the morphology of the nanofibers, scanning electron microscopy was used. Fourier transform infrared spectroscopy (FT-IR), and differential scanning calorimetry (DSC) were applied for the solid-state characterization of the samples, while the drug release profile was followed by the in vitro dissolution test. The nanofibrous formulations had diameters in the range of few hundred nanometers. FT-IR spectra and DSC thermograms indicated the amorphization of aceclofenac, which resulted in a rapid release of the active substance. The characteristics of the selected ternary fiber composition (10 mg/g aceclofenac, 1% / triethanolamine, 15% / PVPK90) were found to be suitable for obtaining orally dissolving webs of fast dissolution and potential oral absorption.
通过静电纺丝制备了载有醋氯芬酸的聚乙烯吡咯烷酮基纳米纤维制剂，以获得载药口腔崩解片，从而提高属于BCS II类的难溶性抗炎活性成分的溶解度和溶解速率。制备了含三乙醇胺的醋氯芬酸-聚乙烯吡咯烷酮纳米纤维三元复合材料，以对药物溶解改善发挥协同作用。改变组成和静电纺丝参数以选择具有最佳纤维特性的纤维样品。使用扫描电子显微镜确定纳米纤维的形态。采用傅里叶变换红外光谱（FT-IR）和差示扫描量热法（DSC）对样品进行固态表征，同时通过体外溶出试验跟踪药物释放曲线。纳米纤维制剂的直径在几百纳米范围内。FT-IR光谱和DSC热谱图表明醋氯芬酸非晶化，这导致活性物质快速释放。发现所选三元纤维组合物（10 mg/g醋氯芬酸、1%三乙醇胺、15% PVPK90）的特性适合获得快速溶解且具有潜在口服吸收性的口腔崩解片。
