Department of Environmental Health Engineering, Faculty of Health and Research Center for Health Sciences, Hamadan University of Medical Sciences, Hamadan 6517838636, Iran.
Faculty of Chemistry, Bu-Ali Sina University, Hamedan 6516738695, Iran.
Int J Mol Sci. 2021 Nov 19;22(22):12479. doi: 10.3390/ijms222212479.
The iontophoresis delivery of insulin (INS) remains a serious challenge due to the low permeability of the drug through the skin. This work aims to investigate the potential of water-soluble polypyrrole nanoparticles (WS-PPyNPs) as a drug donor matrix for controlled transdermal iontophoresis of INS. WS-PPyNPs have been prepared via a simple chemical polymerization in the presence of sodium dodecyl sulfate (SDS) as both dopant and the stabilizing agent. The synthesis of the soluble polymer was characterized using field emission scanning electron microscopy (FESEM), dynamic light scattering (DLS), fluorescence spectroscopy, and Fourier transform infrared (FT-IR) spectroscopy. The loading mechanism of INS onto the WS-PPyNPs is based on the fact that the drug molecules can be replaced with doped dodecyl sulfate. A two-compartment Franz-type diffusion cell was employed to study the effect of current density, formulation pH, INS concentration, and sodium chloride concentration on anodal iontophoresis (AIP) and cathodal iontophoresis (CIP) of INS across the rat skin. Both AIP and CIP delivery of INS using WS-PPyNPs were significantly increased compared to passive delivery. Furthermore, while the AIP experiment (60 min at 0.13 mA cm) show low cumulative drug permeation for INS (about 20.48 µg cm); the CIP stimulation exhibited a cumulative drug permeation of 68.29 µg cm. This improvement is due to the separation of positively charged WS-PPyNPs and negatively charged INS that has occurred in the presence of cathodal stimulation. The obtained results confirm the potential applicability of WS-PPyNPs as an effective approach in the development of controlled transdermal iontophoresis of INS.
由于药物透过皮肤的渗透性低，胰岛素（INS）的离子电渗递药仍然是一个严峻的挑战。本工作旨在研究水溶性聚吡咯纳米粒子（WS-PPyNPs）作为一种药物供体基质，用于控制 INS 的经皮离子电渗递药的潜力。WS-PPyNPs 是通过在存在十二烷基硫酸钠（SDS）作为掺杂剂和稳定剂的情况下，通过简单的化学聚合制备的。使用场发射扫描电子显微镜（FESEM）、动态光散射（DLS）、荧光光谱和傅里叶变换红外（FT-IR）光谱对可溶性聚合物的合成进行了表征。INS 加载到 WS-PPyNPs 上的机制基于这样一个事实，即药物分子可以被掺杂的十二烷基硫酸盐取代。采用双室 Franz 型扩散池研究电流密度、制剂 pH 值、INS 浓度和氯化钠浓度对 INS 经大鼠皮肤进行阳极离子电渗（AIP）和阴极离子电渗（CIP）的影响。与被动传递相比，使用 WS-PPyNPs 的 INS 的 AIP 和 CIP 传递均显著增加。此外，虽然 AIP 实验（0.13 mA cm 下 60 分钟）显示 INS 的累积药物渗透量低（约 20.48 µg cm）；但 CIP 刺激显示出 68.29 µg cm 的累积药物渗透量。这种改进归因于在阴极刺激存在下发生的带正电荷的 WS-PPyNPs 和带负电荷的 INS 的分离。所得结果证实了 WS-PPyNPs 作为开发 INS 经皮离子电渗递药的有效方法的潜在适用性。
