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Absorption-enhancing effects of gemini surfactant on the intestinal absorption of poorly absorbed hydrophilic drugs including peptide and protein drugs in rats.
Int J Pharm. 2016 Feb 29; 499(1-2):58-66.IJ

Abstract

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 isothiocyanate-dextrans (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.

Authors+Show Affiliations

Department of Biopharmaceutics, Kyoto Pharmaceutical University, Misasagi, Yamashina-Ku, Kyoto 607-8414, Japan.Department of Biopharmaceutics, Kyoto Pharmaceutical University, Misasagi, Yamashina-Ku, Kyoto 607-8414, Japan.Department of Biopharmaceutics, Kyoto Pharmaceutical University, Misasagi, Yamashina-Ku, Kyoto 607-8414, Japan.Department of Biopharmaceutics, Kyoto Pharmaceutical University, Misasagi, Yamashina-Ku, Kyoto 607-8414, Japan.Department of Biopharmaceutics, Kyoto Pharmaceutical University, Misasagi, Yamashina-Ku, Kyoto 607-8414, Japan. Electronic address: yamamoto@mb.kyoto-phu.ac.jp.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

26707414

Citation

Alama, Tammam, et al. "Absorption-enhancing Effects of Gemini Surfactant On the Intestinal Absorption of Poorly Absorbed Hydrophilic Drugs Including Peptide and Protein Drugs in Rats." International Journal of Pharmaceutics, vol. 499, no. 1-2, 2016, pp. 58-66.
Alama T, Kusamori K, Katsumi H, et al. Absorption-enhancing effects of gemini surfactant on the intestinal absorption of poorly absorbed hydrophilic drugs including peptide and protein drugs in rats. Int J Pharm. 2016;499(1-2):58-66.
Alama, T., Kusamori, K., Katsumi, H., Sakane, T., & Yamamoto, A. (2016). Absorption-enhancing effects of gemini surfactant on the intestinal absorption of poorly absorbed hydrophilic drugs including peptide and protein drugs in rats. International Journal of Pharmaceutics, 499(1-2), 58-66. https://doi.org/10.1016/j.ijpharm.2015.12.043
Alama T, et al. Absorption-enhancing Effects of Gemini Surfactant On the Intestinal Absorption of Poorly Absorbed Hydrophilic Drugs Including Peptide and Protein Drugs in Rats. Int J Pharm. 2016 Feb 29;499(1-2):58-66. PubMed PMID: 26707414.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Absorption-enhancing effects of gemini surfactant on the intestinal absorption of poorly absorbed hydrophilic drugs including peptide and protein drugs in rats. AU - Alama,Tammam, AU - Kusamori,Kosuke, AU - Katsumi,Hidemasa, AU - Sakane,Toshiyasu, AU - Yamamoto,Akira, Y1 - 2015/12/17/ PY - 2015/10/02/received PY - 2015/11/17/revised PY - 2015/12/14/accepted PY - 2015/12/29/entrez PY - 2015/12/29/pubmed PY - 2016/11/1/medline KW - Absorption enhancer KW - Calcitonin KW - Gemini surfactant KW - Intestinal absorption KW - Peptide drug KW - Poorly absorbed drug SP - 58 EP - 66 JF - International journal of pharmaceutics JO - Int J Pharm VL - 499 IS - 1-2 N2 - 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 isothiocyanate-dextrans (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. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/26707414/Absorption_enhancing_effects_of_gemini_surfactant_on_the_intestinal_absorption_of_poorly_absorbed_hydrophilic_drugs_including_peptide_and_protein_drugs_in_rats_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(15)30441-5 DB - PRIME DP - Unbound Medicine ER -