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Improvement of pulmonary absorptions of poorly absorbable drugs using Gelucire 44/14 as an absorption enhancer.
J Pharm Pharmacol. 2014 Oct; 66(10):1410-20.JP

Abstract

OBJECTIVES

This study aims to evaluate the absorption-enhancing effects of Gelucire 44/14 on the pulmonary absorption of different poorly absorbable drugs and relative mechanism of action.

METHODS

Absorption-enhancing effect of Gelucire 44/14 were examined by an in-vivo pulmonary absorption experiment in rats, and the membrane toxicity of Gelucire 44/14 was evaluated by measuring levels of protein and dehydrogenase (LDH) in the bronchoalveolar lavage fluid (BALF) and morphological observation.

KEY FINDINGS

Pulmonary absorptions of fluorescein isothiocyanate-dextrans, insulin and calcitonin were enhanced by Gelucire 44/14 (0.1-2.0%, w/v) in a concentration-dependent manner, and the maximal absorption-enhancing effect was obtained when the concentration of Gelucire 44/14 increased to 2.0% (w/v). Furthermore, Gelucire 44/14 neither increase the levels of protein and LDH in BALF nor change morphology of lung compared with control group. In addition, a well correlation between the absorption-enhancing effect and surface tension of insulin solution in the presence of Gelucire 44/14 was observed, suggesting Gelucire 44/14-mediated decrease in the surface tension of the gas-liquid interface in alveolar tissue was possible one of the improving mechanisms of Gelucire 44/14.

CONCLUSION

Gelucire 44/14 was a potential and safe absorption enhancer for improving the absorption of poorly absorbable drugs including insulin and calcitonin by pulmonary delivery.

Authors+Show Affiliations

School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an, China.No affiliation info availableNo 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

24849123

Citation

Zhang, Hailong, et al. "Improvement of Pulmonary Absorptions of Poorly Absorbable Drugs Using Gelucire 44/14 as an Absorption Enhancer." The Journal of Pharmacy and Pharmacology, vol. 66, no. 10, 2014, pp. 1410-20.
Zhang H, Huang X, Mi J, et al. Improvement of pulmonary absorptions of poorly absorbable drugs using Gelucire 44/14 as an absorption enhancer. J Pharm Pharmacol. 2014;66(10):1410-20.
Zhang, H., Huang, X., Mi, J., Huo, Y., Wang, G., Xing, J., & Gao, Y. (2014). Improvement of pulmonary absorptions of poorly absorbable drugs using Gelucire 44/14 as an absorption enhancer. The Journal of Pharmacy and Pharmacology, 66(10), 1410-20. https://doi.org/10.1111/jphp.12274
Zhang H, et al. Improvement of Pulmonary Absorptions of Poorly Absorbable Drugs Using Gelucire 44/14 as an Absorption Enhancer. J Pharm Pharmacol. 2014;66(10):1410-20. PubMed PMID: 24849123.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Improvement of pulmonary absorptions of poorly absorbable drugs using Gelucire 44/14 as an absorption enhancer. AU - Zhang,Hailong, AU - Huang,Xiaoyan, AU - Mi,Jie, AU - Huo,Yayu, AU - Wang,Guan, AU - Xing,Jianfeng, AU - Gao,Yang, Y1 - 2014/05/22/ PY - 2013/12/05/received PY - 2014/04/13/accepted PY - 2014/5/23/entrez PY - 2014/5/23/pubmed PY - 2015/6/3/medline KW - Gelucire 44/14 KW - absorption enhancer KW - membrane toxicity KW - poorly absorbable drugs KW - pulmonary absorption SP - 1410 EP - 20 JF - The Journal of pharmacy and pharmacology JO - J Pharm Pharmacol VL - 66 IS - 10 N2 - OBJECTIVES: This study aims to evaluate the absorption-enhancing effects of Gelucire 44/14 on the pulmonary absorption of different poorly absorbable drugs and relative mechanism of action. METHODS: Absorption-enhancing effect of Gelucire 44/14 were examined by an in-vivo pulmonary absorption experiment in rats, and the membrane toxicity of Gelucire 44/14 was evaluated by measuring levels of protein and dehydrogenase (LDH) in the bronchoalveolar lavage fluid (BALF) and morphological observation. KEY FINDINGS: Pulmonary absorptions of fluorescein isothiocyanate-dextrans, insulin and calcitonin were enhanced by Gelucire 44/14 (0.1-2.0%, w/v) in a concentration-dependent manner, and the maximal absorption-enhancing effect was obtained when the concentration of Gelucire 44/14 increased to 2.0% (w/v). Furthermore, Gelucire 44/14 neither increase the levels of protein and LDH in BALF nor change morphology of lung compared with control group. In addition, a well correlation between the absorption-enhancing effect and surface tension of insulin solution in the presence of Gelucire 44/14 was observed, suggesting Gelucire 44/14-mediated decrease in the surface tension of the gas-liquid interface in alveolar tissue was possible one of the improving mechanisms of Gelucire 44/14. CONCLUSION: Gelucire 44/14 was a potential and safe absorption enhancer for improving the absorption of poorly absorbable drugs including insulin and calcitonin by pulmonary delivery. SN - 2042-7158 UR - https://www.unboundmedicine.com/medline/citation/24849123/Improvement_of_pulmonary_absorptions_of_poorly_absorbable_drugs_using_Gelucire_44/14_as_an_absorption_enhancer_ L2 - https://doi.org/10.1111/jphp.12274 DB - PRIME DP - Unbound Medicine ER -