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Improvement of pulmonary absorption of insulin and other water-soluble compounds by polyamines in rats.
J Control Release. 2007 Sep 11; 122(1):94-101.JC

Abstract

The absorption enhancing effects of polyamines, spermine (SPM), spermidine (SPD) and putrescine (PUT) on the pulmonary absorption of poorly absorbable drugs were studied in rats. Insulin, 5(6)-carboxyfluorescein (CF), and fluorescein isothiocyanate-labeled dextrans (FDs) were chosen as models of poorly absorbable drugs. The absorption of insulin from the lung was enhanced in the presence of SPM and SPD, while PUT had almost no absorption enhancing effect for improving the pulmonary absorption of insulin in rats. SPM also improved the pulmonary absorption of FDs with various molecular weights, although we found almost no significant difference in the pulmonary absorption of CF with or without SPM. As for the pulmonary membrane toxicity of SPM, there was no significant difference in the release of protein and lactate dehydrogenase (LDH) with or without SPM in bronchoalveolar lavage fluid (BALF), indicating that SPM did not cause any membrane damage to the lung tissues. Furthermore, SPM did not affect the stability of insulin in BALF, suggesting that SPM might increase the permeability of insulin across the alveolar epithelium. In conclusion, polyamines, especially SPM can effectively improve the pulmonary absorption of insulin and other macromolecules without any membrane damage to the lung tissues.

Authors+Show Affiliations

Department of Biopharmaceutics, Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Kyoto, Japan.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

17651854

Citation

He, Lin, et al. "Improvement of Pulmonary Absorption of Insulin and Other Water-soluble Compounds By Polyamines in Rats." Journal of Controlled Release : Official Journal of the Controlled Release Society, vol. 122, no. 1, 2007, pp. 94-101.
He L, Gao Y, Lin Y, et al. Improvement of pulmonary absorption of insulin and other water-soluble compounds by polyamines in rats. J Control Release. 2007;122(1):94-101.
He, L., Gao, Y., Lin, Y., Katsumi, H., Fujita, T., & Yamamoto, A. (2007). Improvement of pulmonary absorption of insulin and other water-soluble compounds by polyamines in rats. Journal of Controlled Release : Official Journal of the Controlled Release Society, 122(1), 94-101.
He L, et al. Improvement of Pulmonary Absorption of Insulin and Other Water-soluble Compounds By Polyamines in Rats. J Control Release. 2007 Sep 11;122(1):94-101. PubMed PMID: 17651854.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Improvement of pulmonary absorption of insulin and other water-soluble compounds by polyamines in rats. AU - He,Lin, AU - Gao,Yang, AU - Lin,Yulian, AU - Katsumi,Hidemasa, AU - Fujita,Takuya, AU - Yamamoto,Akira, Y1 - 2007/06/27/ PY - 2007/02/22/received PY - 2007/05/06/revised PY - 2007/06/19/accepted PY - 2007/7/27/pubmed PY - 2007/10/17/medline PY - 2007/7/27/entrez SP - 94 EP - 101 JF - Journal of controlled release : official journal of the Controlled Release Society JO - J Control Release VL - 122 IS - 1 N2 - The absorption enhancing effects of polyamines, spermine (SPM), spermidine (SPD) and putrescine (PUT) on the pulmonary absorption of poorly absorbable drugs were studied in rats. Insulin, 5(6)-carboxyfluorescein (CF), and fluorescein isothiocyanate-labeled dextrans (FDs) were chosen as models of poorly absorbable drugs. The absorption of insulin from the lung was enhanced in the presence of SPM and SPD, while PUT had almost no absorption enhancing effect for improving the pulmonary absorption of insulin in rats. SPM also improved the pulmonary absorption of FDs with various molecular weights, although we found almost no significant difference in the pulmonary absorption of CF with or without SPM. As for the pulmonary membrane toxicity of SPM, there was no significant difference in the release of protein and lactate dehydrogenase (LDH) with or without SPM in bronchoalveolar lavage fluid (BALF), indicating that SPM did not cause any membrane damage to the lung tissues. Furthermore, SPM did not affect the stability of insulin in BALF, suggesting that SPM might increase the permeability of insulin across the alveolar epithelium. In conclusion, polyamines, especially SPM can effectively improve the pulmonary absorption of insulin and other macromolecules without any membrane damage to the lung tissues. SN - 1873-4995 UR - https://www.unboundmedicine.com/medline/citation/17651854/Improvement_of_pulmonary_absorption_of_insulin_and_other_water_soluble_compounds_by_polyamines_in_rats_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0168-3659(07)00304-5 DB - PRIME DP - Unbound Medicine ER -