Absorption-enhancing effects of gemini surfactant on the intestinal absorption of poorly absorbed hydrophilic drugs including peptide and protein drugs in rats

被引:25
|
作者
Alama, Tammam [1 ]
Kusamori, Kosuke [1 ]
Katsumi, Hidemasa [1 ]
Sakane, Toshiyasu [1 ]
Yamamoto, Akira [1 ]
机构
[1] Kyoto Pharmaceut Univ, Dept Biopharmaceut, Yamashina Ku, Kyoto 6078414, Japan
关键词
Intestinal absorption; Absorption enhancer; Gemini surfactant; Poorly absorbed drug; Peptide drug; Calcitonin; COLON-SPECIFIC DELIVERY; NITRIC-OXIDE DONORS; PERMEABILITY CHARACTERISTICS; LIPOPHILIC DERIVATIVES; CHEMICAL-MODIFICATION; LEUCINE-ENKEPHALIN; CHITOSAN CAPSULES; MUCOSAL TOXICITY; FATTY-ACIDS; PHENOL RED;
D O I
10.1016/j.ijpharm.2015.12.043
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In general, the intestinal absorption of small hydrophilic molecules and macromolecules like peptides, after oral administration is very poor. Absorption enhancers are considered to be one of the most promising agents to enhance the intestinal absorption of drugs. In this research, we focused on a gemini surfactant, a new type of absorption enhancer. The intestinal absorption of drugs, with or without sodium dilauramidoglutamide lysine (SLG-30), a gemini surfactant, was examined by an in situ closed-loop method in rats. The intestinal absorption of 5(6)-carboxyfluorescein (CF) and fluorescein isothiocyanatedextrans (FDs) was significantly enhanced in the presence of SLG-30, such effect being reversible. Furthermore, the calcium levels in the plasma significantly decreased when calcitonin was co-administered with SLG-30, suggestive of the increased intestinal absorption of calcitonin. In addition, no significant increase in the of lactate dehydrogenase (LDH) activity or in protein release from the intestinal epithelium was observed in the presence of SLG-30, suggestive of the safety of this compound. These findings indicate that SLG-30 is an effective absorption-enhancer for improving the intestinal absorption of poorly absorbed drugs, without causing serious damage to the intestinal epithelium. (C) 2015 Elsevier B.V. All rights reserved.
引用
收藏
页码:58 / 66
页数:9
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