Modulation of gastrointestinal permeability of low-molecular-weight heparin by L-arginine: in-vivo and in-vitro evaluation.

The Journal of Pharmacy and Pharmacology
Nusrat A MotlekarBi-Botti C Youan

Abstract

L-Arginine is the principal physiological precursor of nitric oxide (NO, a key neurotransmitter) that plays a versatile role in the physiology of the gastrointestinal tract. In this study, the efficacy of L-arginine in enhancing intestinal absorption of ardeparin, a low-molecular-weight heparin (LMWH) was investigated in Caco-2 cell monolayers and a rat model. Regional permeability studies using rat intestine were performed using a modified Ussing chamber. Cell viability in the presence of various concentrations of enhancer was determined by MTT assay. Furthermore, the eventual mucosal epithelial damage was histologically evaluated. LMWH formulated with L-arginine was administered orally to male Sprague-Dawley rats and the absorption of LMWH was determined by measuring plasma anti-factor Xa activity. Higher ardeparin in-vitro permeability (approximately 3 fold) compared with control was observed in the presence of 2% L-arginine. Regional permeability studies indicated predominant absorption in the colon region. Cell viability studies showed no significant cytotoxicity below 0.8% L-arginine. The oral bioavailability of ardeparin formulated with L-arginine (250 mg kg(-1)) was increased by approximately 2 fold compared with contro...Continue Reading

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Citations

Dec 14, 2011·International Journal of Nanomedicine·Alyaa RamadanJean Pierre Benoit
Nov 26, 2009·Drug Development and Industrial Pharmacy·Julien Scala-BertolaPhilippe Maincent
Oct 23, 2010·Experimental and Molecular Pathology·Zhanna ServetnykAnca Dragomir
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Jul 2, 2016·Pharmaceuticals·Ana Rita NevesMadalena Pinto
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Jan 6, 2010·The Journal of Bone and Joint Surgery. American Volume·Daniel DavisFelix H Savoie
Nov 21, 2018·Current Medicinal Chemistry·Daniel K Afosah, Rami A Al-Horani
Feb 6, 2020·AAPS PharmSciTech·Nermin E ElerakyGiovanni M Pauletti
May 22, 2007·The Journal of Nutrition·Yvette C Luiking, Nicolaas E P Deutz

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