Salcaprozate sodium

Salcaprozate sodium (SNAC), an oral absorption promoter, and has the potential as a delivery agent for oral forms of heparin and insulin. Salcaprozate sodium could increase passive transcellular permeation across small intestinal epithelia based on increased lipophilicity arising from non-covalent macromolecule complexation[1][2].

SNAC (12.5-400 μg/mL; 24 h) has no toxicity to Caco-2 cells, and the survival percentage is above 90% when SNAC is 200 μg/mL[3].SNAC (50 and 200 μg/mL) improves the apparent permeability coeffcient (Papp) of RA and SA-B by 2.14-fold and 3.68-fold compared with the Papp of SAs solution[3].

SNAC improves the oral absorption of both R1 and SAs and enhances bioavailability in rats[3].SNAC (2000 mg/kg/d; oral gavage for 13 weeks) related mortality is evident only at the 2000-mg/kg/d level, 20% among males and 50% among females; no clear cause of death is evident[1].SNAC (100-1000 mg/kg/d; oral gavage for 13 weeks) induces no mortality in the Wistar rat study at doses up to 1000 mg/kg/d[1]. Animal Model: Sprague-Dawley rats (6-7 weeks)[1]

[1]. Riley MGI, et, al. Subchronic oral toxicity of salcaprozate sodium (SNAC) in Sprague-Dawley and Wistar rats. Int J Toxicol. Jul-Aug 2009; 28(4):278-93. [2]. Twarog C, et, al. Intestinal Permeation Enhancers for Oral Delivery of Macromolecules: A Comparison between Salcaprozate Sodium (SNAC) and Sodium Caprate (C 10). Pharmaceutics. 2019 Feb 13; 11(2):78. [3]. Li Y, et, al. Impact of Sodium N-[8-(2-Hydroxybenzoyl)amino]-caprylate on Intestinal Permeability for Notoginsenoside R1 and Salvianolic Acids in Caco-2 Cells Transport and Rat Pharmacokinetics. Molecules. 2018 Nov 16; 23(11):2990.