Kim, SK Kim, K Lee, S Park, K Park, JH Kwon, IC Choi, K Kim, CY Byun, Y 2024-01-21T04:10:26Z 2024-01-21T04:10:26Z 2021-09-03 2005-10-04 0731-7085 https://pubs.kist.re.kr/handle/201004/136058 We validated the application of the surface plasmon resonance (SPR) technique to reliably determine adhesion of drugs to the intestinal wall using heparin-DOCA conjugates, developed to enhance the oral absorption of poorly absorbed heparin. In this study, heparin conjugates, or deoxycholyl-heparin (H-DOCA) and bisdeoxycholyl-heparin (H-bis-DOCA), were synthesized by covalently coupling the synthesized succinimido deoxycholate (DOCA-NHS) or succinimido bis-deoxycholyl-L-lysine (DOCA-bis-NHS) to amine groups of heparin, and their physicochemical and biological properties were evaluated. To mimic the duodenal and ileal surfaces, duodenal and ileal brush border membrane (BBM) vesicles isolated from Sprauge-Dawley (SD) rats were immobilized onto a biosensor chip composed of dextran derivatives with modified lipophilic residues. The adhesion of heparin conjugates on the BBM surface was evaluated by measuring the SPR response signal. The adhesion of heparin conjugates was significantly dependent on the conjugated DOCA molecules: that is, they showed higher adhesion signal on the ilea] BBM surface than that on the duodenal BBM surface. In particular, the solubilized heparin conjugates in DMSO solution presented significantly increased adhesion affinity on the ileal 1313M surface. The adhesion of heparin conjugates on the intestinal surfaces was successfully assayed using the surface plasmon resonance technique with the sensor chip on which BBM vesicles were immobilized. (c) 2005 Elsevier B.V. All rights reserved. English ELSEVIER MOLECULAR-WEIGHT HEPARIN BRUSH-BORDER MEMBRANES BIOSENSOR DERIVATIVES Evaluation of absorption of heparin-DOCA conjugates on the intestinal wall using a surface plasmon resonance Article 10.1016/j.jpba.2005.06.014 1 JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, v.39, no.5, pp.861 - 870 JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS 39 5 861 870 scie scopus 000233067000002 2-s2.0-26644447763 Chemistry, Analytical Pharmacology & Pharmacy Chemistry Pharmacology & Pharmacy Article MOLECULAR-WEIGHT HEPARIN BRUSH-BORDER MEMBRANES BIOSENSOR DERIVATIVES heparin deoxycholic acid surface plasmon resonance brush border membrane