아테놀롤의 비강 및 장관 투과에 대한 C-말단 변형 밀착결합 조절제와 프룩토스 폴리머의 영향

Effect of C-terminal Amidated Tight Junction Modulator and Fructose Polymer on the Nasal and Intestinal Permeation of Atenolol

Zonula occludens toxin has been shown to reversibly open tight junctions in endothelial and epithelial cells. The purpose of this study was to evaluate the permeation activity of C-terminal amidated fragment of Zonula occludens toxin and co-administration with a fructose polymer on enhancing the nasal and duodenal administration of atenolol. The C-terminal amidated peptide (Phe-Cys-Ile-Gly-Arg-Leu-NH2) resulted in statistically significant improvement in permeation of atenolol compared to the control in both nasal and duodenal administration. Also, the permeability enhancing effect of the C-terminal amidated peptide was significantly promoted by the fructose polymer, levan. C-terminal amidated peptide together with the addition of levan may be promising as a tight junction modulated permeation enhancer, and allow the development of the mucosal drug delivery of low bioavailability therapeutic agents.