Enhanced transbuccal salmon calcitonin (sCT) delivery: Effect of chemical enhancers and electrical assistance on in vitro sCT buccal permeation

This study investigates the combined effect of absorption enhancers and electrical assistance on transbuccal salmon calcitonin (sCT) delivery, using fresh swine buccal tissue. We placed 200 IU (40 μg/mL) of each sCT formulation—containing various concentrations of ethanol, N-acetyl-l-cysteine (NAC), and sodium deoxyglycocholate (SDGC)—onto the donor part of a Franz diffusion cell. Then, 0.5 mA/cm2 of fixed anodal current was applied alone or combined with chemical enhancers. The amount of permeated sCT was analyzed using an ELISA kit, and biophysical changes of the buccal mucosa were investigated using FT-IR spectroscopy, and hematoxylin–eosin staining methods were used to evaluate histological alteration of the buccal tissues. The flux (Js) of sCT increased with the addition of absorption enhancer groups, but it was significantly enhanced by the application of anodal iontophoresis (ITP). FT-IR study revealed that all groups caused an increase in lipid fluidity but only the groups containing SDGC showed statistically significant difference. Although the histological data of SDGC groups showed a possibility for tissue damage, the present enhancing methods appear to be safe. In conclusion, the combination of absorption enhancers and electrical assistance is a potential strategy for the enhancement of transbuccal sCT delivery.

Graphical abstractThe flux (Js) of sCT was increased by the aid of absorption enhancers and iontophoresis. However Js of transbuccal sCT was more enhanced by the combination of absorption enhancers and electrical assistance.Figure optionsDownload full-size imageDownload as PowerPoint slide