In vitro bioadhesion of carbohydrate-containing N-(2-hydroxypropyl) methacrylamide copolymers to the GI tract of guinea pigs

作者: Blanka Říhová , Ramesh C. Rathi , Pavla Kopečková , Jindřich Kopeček

DOI: 10.1016/0378-5173(92)90233-R

关键词: Small intestineMannosamineFucoseChemistryGalactosamineGuinea pigN-(2-Hydroxypropyl) methacrylamideGlucosamineMethacrylamideBiochemistry

摘要: Abstract N-(2-Hydroxypropyl)methacrylamide (HPMA) copolymers with different content of pendant saccharide moieties (galactosamine, fucosylamine, glucosamine, mannosamine) were synthesized and their bioadhesive properties to the gastrointestinal (GI) tract female adult guinea pigs have been studied in vitro. Radioiodinated HPMA incubated everted sacs or enterocytes isolated from pig small intestine colon. The results obtained clearly indicated preferential binding fucosylamine containing colonic mucus. extent increased increasing time incubation, decreased molecular weight copolymers. was partially inhibited by presence free fucose glucose incubation medium. Fucosylamine also bind increases Contrary on sacs, there no difference either indicate lectine-like structures GI tract.

参考文章(42)
E.C. Beyer, S.E. Zweig, S.H. Barondes, Two lactose binding lectins from chicken tissues. Purified lectin from intestine is different from those in liver and muscle. Journal of Biological Chemistry. ,vol. 255, pp. 4236- 4239 ,(1980) , 10.1016/S0021-9258(19)85657-0
A. B. R. Thomson, J. M. Dietschy, The Role of the Unstirred Water Layer in Intestinal Permeation Springer, Berlin, Heidelberg. pp. 165- 269 ,(1984) , 10.1007/978-3-642-69508-7_4
M. J. Humphrey, The Oral Bioavailability of Peptides and Related Drugs Springer, Boston, MA. pp. 139- 151 ,(1986) , 10.1007/978-1-4757-9960-6_11
Adrian Allen, David A. Hutton, Jeffrey P. Pearson, Lynda A. Sellers, Mucus glycoprotein structure, gel formation and gastrointestinal mucus function Ciba Foundation symposium. ,vol. 109, pp. 137- 156 ,(1984) , 10.1002/9780470720905.CH10
Leung S.H.S., J M Gu, J R Robinson, BINDING OF ACRYLIC POLYMERS TO MUCIN/EPITHELIAL SURFACES: STRUCTURE - PROPERTY RELATIONSHIPS Critical Reviews in Therapeutic Drug Carrier Systems. ,vol. 5, pp. 21- 67 ,(1988)
Susan A. Cartlidge, Ruth Duncan, John B. Lloyd, Pavla Kopečková—Rejmanová, Jindřich Kopeček, Soluble, crosslinked N-(2-hydroxypropyl)methacrylamide copolymers as potential drug carriers. 3. Targeting by incorporation of galactosamine residues. Effect of route of administration Journal of Controlled Release. ,vol. 4, pp. 265- 278 ,(1987) , 10.1016/0168-3659(87)90018-6
M Izhar, Y Nuchamowitz, D Mirelman, Adherence of Shigella flexneri to guinea pig intestinal cells is mediated by a mucosal adhesion. Infection and Immunity. ,vol. 35, pp. 1110- 1118 ,(1982) , 10.1128/IAI.35.3.1110-1118.1982
Pavla Kopečková, Jindřich Kopeček, Release of 5‐aminosalicylic acid from bioadhesive N‐(2‐hydroxypropyl)methacrylamide copolymers by azoreductases in vitro Macromolecular Chemistry and Physics. ,vol. 191, pp. 2037- 2045 ,(1990) , 10.1002/MACP.1990.021910906
Janine F. Bridges, John F. Woodley, Ruth Duncan, Jindr̆ich Kopec̆ek, Soluble N-(2-hydroxypropyl) methacrylamide copolymers as a potential oral, controlled-release, drug delivery system. I. Bioadhesion to the rat intestine in vitro International Journal of Pharmaceutics. ,vol. 44, pp. 213- 223 ,(1988) , 10.1016/0378-5173(88)90118-4