Division of Pharmaceutical Sciences, College of Pharmacy, University of Cincinnati, 231 Albert Sabin Way, MSB # 3005, Cincinnati, OH, 45267-0514, USA.
Division of Oral and Maxillofacial Surgery, College of Medicine, University of Cincinnati, Cincinnati, OH, 45267, USA.
Pharm Res. 2023 Aug;40(8):1977-1987. doi: 10.1007/s11095-023-03535-8. Epub 2023 May 31.
Iontophoresis is a noninvasive method that enhances drug delivery using an electric field. This method can improve drug delivery to the tissues in the oral cavity. The effects of iontophoresis on gingival drug delivery have not been investigated. The objectives of this study were to (a) determine the flux enhancement of model permeants across porcine and human gingiva during iontophoresis, (b) examine the transport mechanisms of gingival iontophoresis, and (c) evaluate the potential of iontophoretically enhanced delivery for three model drugs lidocaine, ketorolac, and chlorhexidine.
Passive and iontophoretic fluxes were determined with porcine and human gingiva using a modified Franz diffusion cell and model drugs and permeants. To investigate the transport mechanisms of iontophoresis, the enhancement from the direct-field effect was determined by positively and negatively charged model permeants. The electroosmosis enhancement effect was determined with neutral permeants of different molecular weight. The alteration of the gingival barrier due to electropermeabilization was evaluated using electrical resistance measurements.
Significant flux enhancement was observed during gingival iontophoresis. The direct-field effect was the major mechanism governing the iontophoretic transport of the charged permeants. Electroosmosis was from anode to cathode. The effective pore radius of the iontophoretic transport pathways in the porcine gingiva was ~0.68 nm. Irreversible electropermeabilization was observed after 2 and 4 h of iontophoresis under the conditions studied.
Iontophoresis could enhance drug delivery and reduce transport lag time, showing promise for gingival drug delivery.
电渗析是一种非侵入性方法，利用电场增强药物输送。这种方法可以改善药物在口腔组织中的输送。电渗析对牙龈药物输送的影响尚未得到研究。本研究的目的是：（a）确定模型渗透物在电渗析过程中穿过猪和人牙龈的通量增强，（b）研究牙龈电渗析的传输机制，以及（c）评估三种模型药物利多卡因、酮咯酸和洗必泰经离子电渗增强输送的潜力。
使用改良的 Franz 扩散池和模型药物和渗透物，通过猪和人牙龈确定被动和电渗析通量。为了研究电渗析的传输机制，通过带正电荷和负电荷的模型渗透物确定直接电场效应的增强。用不同分子量的中性渗透物确定电渗增强效应。通过电阻测量评估由于电穿孔而对牙龈屏障的改变。
在牙龈电渗析过程中观察到明显的通量增强。直接电场效应是带电渗透物电渗传输的主要机制。电渗是从阳极到阴极。在研究条件下，电渗 2 和 4 小时后，观察到不可逆的电穿孔。
电渗析可以增强药物输送并减少传输滞后时间，为牙龈药物输送带来希望。
