Teno Jorge, Evtoski Zoran, Prieto Cristina, Lagaron Jose M
R&D Department, Bionanopharma S.L., Calle Algepser 65 nave 3, 46980 Paterna, Valencia, Spain.
Novel Materials and Nanotechnology Group, Institute of Agrochemistry and Food Technology (IATA), Spanish Council for Scientific Research (CSIC), Calle Catedrático Agustín Escardino Benlloch 7, 46980 Paterna, Valencia, Spain.
Pharmaceutics. 2025 Jul 16;17(7):921. doi: 10.3390/pharmaceutics17070921.
: The work presented herein focused on the development and characterization of a transdermal caffeine platform fabricated from ultrathin micro- and submicron fibers produced via electrospinning. : The formulations incorporated caffeine encapsulated in a polyethylene oxide (PEO) matrix, combined with various permeation enhancers. A backing layer made of annealed electrospun polycaprolactone (PCL) facilitated the lamination of the two layers to form the final multilayer patch. Comprehensive characterization was conducted, utilizing scanning electron microscopy (SEM) to assess the fiber morphology, attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR) for chemical detection and to assess the stability of the caffeine, and differential scanning calorimetry (DSC) along with wide-angle X-ray scattering (WAXS) to analyze the physical state of the caffeine within the fibers of the active layer. Additionally, Franz cell permeation studies were performed using both synthetic membranes (Strat-M) and ex vivo human stratum corneum (SC) to evaluate and model the permeation kinetics. These experiments demonstrated the significant role of enhancers in modulating the caffeine permeation rates provided by the patch, achieving permeation rates of up to 0.73 mg/cm within 24 h. This work highlights the potential of using electro-hydrodynamic processing technology to develop innovative transdermal delivery systems for drugs, offering a promising strategy for enhancing efficacy and innovative therapeutic direct plasma administration.
本文所展示的工作聚焦于一种经皮咖啡因平台的开发与特性研究，该平台由通过静电纺丝制备的超薄微米和亚微米纤维制成。这些制剂包含包裹在聚环氧乙烷（PEO）基质中的咖啡因，并与各种渗透促进剂相结合。由退火静电纺丝聚己内酯（PCL）制成的背衬层有助于两层的层压，以形成最终的多层贴片。进行了全面的特性表征，利用扫描电子显微镜（SEM）评估纤维形态，利用衰减全反射傅里叶变换红外光谱（ATR-FTIR）进行化学检测并评估咖啡因的稳定性，利用差示扫描量热法（DSC）以及广角X射线散射（WAXS）分析活性层纤维中咖啡因的物理状态。此外，使用合成膜（Strat-M）和离体人角质层（SC）进行了Franz细胞渗透研究，以评估和模拟渗透动力学。这些实验证明了渗透促进剂在调节贴片提供的咖啡因渗透速率方面的重要作用，在24小时内实现了高达0.73毫克/平方厘米的渗透速率。这项工作突出了利用电流体动力学加工技术开发创新型药物经皮给药系统的潜力，为提高疗效和创新治疗直接血浆给药提供了一种有前景的策略。
