Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan.
Department of Chemical Engineering, Faculty of Engineering, Jordan University of Science and Technology, Irbid, Jordan.
AAPS PharmSciTech. 2022 Jan 10;23(1):51. doi: 10.1208/s12249-021-02204-6.
Nanofibers have many promising biomedical applications. They can be used for designing transdermal and dermal drug delivery systems. This project aimed to prepare and characterize polyvinylpyrrolidone-based nanofibers as a dermal and transdermal drug delivery system using pioglitazone. Pioglitazone is an oral antidiabetic drug. In addition, it can act as an inflammatory process modulator, making it a good candidate for managing different skin inflammatory conditions such as atopic dermatitis, skin ulcers, and diabetic foot wound healing. Several nanofiber formulations were prepared using the electrospinning method at different drug loadings, polyvinylpyrrolidone concentrations, and flow rates. A cast film with the exact composition of selected nanofiber formulations was prepared as a control. Nanofibers were characterized using a scanning electron microscope to calculate the diameter. Fourier-transform infrared spectroscopy, differential scanning calorimetry, thermogravimetric analysis, and powder X-ray diffraction were performed for physical and biochemical characterizations. In vitro release, drug loading efficiency, and swelling studies were performed. Ex vivo permeation studies were performed using Franz diffusion cells with or without applying a solid microneedle roller. Round uniform nanofibers with a smooth surface were obtained. The diameter of nanofibers was affected by the drug loading and polymer concentration. Fourier-transform infrared spectra showed a potential physical interaction between the drug and the polymer. According to X-ray diffraction, pioglitazone existed in an amorphous form in prepared nanofibers, with partial crystallinity in the casted film. Nanofibers showed a higher swelling rate compared to the casted film. The drug dissolution rate for nanofibers was 2.3-folds higher than the casted films. The polymer concentration affected the drug dissolution rate for nanofibers; however, drug loading and flow rate did not affect the drug dissolution rate for nanofibers. The application of solid microneedles slightly enhances the total amount of drug permeation. However, it did not affect the flux of the drug through the separated epidermis layer for pioglitazone. The drug permeation flux in nanofibers was approximately five times higher than the flux of the casted film. It was observed that pioglitazone is highly retained in skin layers. Graphical abstract.
纳米纤维在许多有前途的生物医学应用中都有应用。它们可用于设计透皮和真皮药物传递系统。本项目旨在使用吡格列酮制备和表征基于聚乙烯吡咯烷酮的纳米纤维作为一种透皮和真皮药物传递系统。吡格列酮是一种口服抗糖尿病药物。此外，它还可以作为炎症过程调节剂，使其成为治疗特应性皮炎、皮肤溃疡和糖尿病足伤口愈合等不同皮肤炎症疾病的良好候选药物。使用电纺法在不同的药物载药量、聚乙烯吡咯烷酮浓度和流速下制备了几种纳米纤维制剂。还制备了具有所选纳米纤维制剂精确组成的铸膜作为对照。使用扫描电子显微镜对纳米纤维进行了表征，以计算直径。进行了傅里叶变换红外光谱、差示扫描量热法、热重分析和粉末 X 射线衍射，以进行物理和生化特性分析。进行了体外释放、药物负载效率和溶胀研究。使用 Franz 扩散池进行了体外渗透研究，其中包括或不包括施加固体微针滚轮。得到了圆形均匀的纳米纤维，表面光滑。纳米纤维的直径受药物载药量和聚合物浓度的影响。傅里叶变换红外光谱表明药物和聚合物之间存在潜在的物理相互作用。根据 X 射线衍射，吡格列酮在制备的纳米纤维中以无定形形式存在，在铸膜中具有部分结晶度。纳米纤维的溶胀率高于铸膜。纳米纤维的药物溶出速率比铸膜高 2.3 倍。聚合物浓度影响纳米纤维的药物溶出速率；然而，药物载药量和流速不影响纳米纤维的药物溶出速率。固体微针的应用略微提高了药物总渗透量。然而，它并没有影响吡格列酮通过分离的表皮层的药物通量。纳米纤维中的药物渗透通量大约是铸膜的五倍。观察到吡格列酮在皮肤层中高度保留。
