Intraduodenal absorption of the new UF- heparin salt ITF 1057 in the conscious dog

Conjugation of Low-Molecular-Weight Heparin and Deoxycholic Acid for the Development of a New Oral Anticoagulant Agent

“…6 To facilitate heparin absorption in the GI tract, several forms of heparin dosage have been developed, such as liposomes, complexes of heparin with hydrophobic organic bases, enteric coating, and aerosol formulation. [7][8][9][10] There also have been attempts to evaluate the enhancing effect of EDTA, acidic buffer, or sulfated surfactants on heparin absorption in the GI tract. 11 Recently, sodium N- [8-(2-hydroxybenzoyl)amino] caprylate (SNAC) and sodium N-[10-(2-hydroxybenzoyl)amino] decanoate (SNAD) were developed as potent promoters of heparin absorption in the GI tract.…”

Antiangiogenic Activity of Orally Absorbable Heparin Derivative in Different Types of Cancer Cells

“…Various approach types, such as liposomes, enteric coatings and enhancers, have been studied for oral absorption of heparin (20)(21)(22)(23): in our previous reports, we developed an orally absorbable low-molecularweight-heparin (LMWH)-deoxycholic acid conjugate, or LHD, by covalently bonding the amine group of N-deoxycholylethylenediamine (DOCA-NH 2 ) with the carboxylic acids of heparin via amide linkage (Fig. 1A) (24).…”

Papain: An Effective Permeation Enhancer for Orally Administered Low Molecular Weight Heparin

“…Although LMWHs are smaller and less charged than unfractionated heparins (UFH), their permeation through the intestinal epithelium is limited and they are not able to reach the blood circulation without support of auxiliary agents. Different approaches have been proposed to increase heparin absorption across intestinal tract such as use of absorption enhancers (1,2) and different carrier systems (3) The reason for diminished or lacking absorption of heparin can be characterized by two biological barriers namely mucus gel layer on the surface of epithelial cells and extracellular matrix (4). On the one hand, mucus gel layer covering epithelia is mainly based on glycoproteins having a linear protein core and cysteine-rich subdomains (4) building up a three-dimensional network which has to be overcome by LMWH in order to reach the absorption membrane.…”