Department of Smart Foods and Drugs, Inje University, Gyeongnam, Republic of Korea.
Eur J Pharm Biopharm. 2011 Oct;79(2):357-63. doi: 10.1016/j.ejpb.2011.05.010. Epub 2011 Jun 12.
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/cm(2) 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 (J(s)) 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.
本研究使用新鲜猪颊黏膜，考察了吸收促进剂与电辅助对鲑鱼降钙素（sCT）经颊给药的联合作用。我们将含有不同浓度乙醇、N-乙酰-L-半胱氨酸（NAC）和脱氧胆酸钠（SDGC）的各 200IU（40μg/mL）sCT 制剂置于 Franz 扩散池的供体部分上。然后，单独或结合化学增强剂施加 0.5mA/cm2 的固定阳极电流。使用 ELISA 试剂盒分析渗透的 sCT 量，并使用傅里叶变换红外（FT-IR）光谱法研究颊黏膜的生物物理变化，使用苏木精-伊红（H&E）染色法评估颊组织的组织学改变。随着吸收促进剂组的加入，sCT 的通量（J(s)）增加，但阳极离子电渗（ITP）的应用显著增强了它。FT-IR 研究表明，所有组都导致脂质流动性增加，但只有含有 SDGC 的组显示出统计学上的显著差异。尽管 SDGC 组的组织学数据显示出组织损伤的可能性，但目前的增强方法似乎是安全的。总之，吸收促进剂和电辅助的联合是增强 sCT 经颊给药的一种有潜力的策略。
