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Design of Lysosomotropic Macromolecular Prodrug of Doxorubicin Using N-Acetyl-α-1,4-Polygalactosamine as a Targeting Carrier to Hepatoma Tissue
- Source :
- Journal of Bioactive and Compatible Polymers; October 1998, Vol. 13 Issue: 4 p257-269, 13p
- Publication Year :
- 1998
-
Abstract
- α-1,4-Polygalactosamine (PGA) and N-acetylated α-1,4-polygalactosamine (NAPGA) are chitosan- and chitin-like biodegradable α-1,4-linked polysaccharides, respectively. Radioactivity of 14C-50% N-acetylated PGA injected into hepatomized mice, was found to accumulate more in the liver, kidney, ileum and hepatoma tumor tissues, compared with other organs. To provide a lysosomotropic macromolecular prodrug of doxorubicin (DXR) targeted to hepatoma tumor tissue, DXR was immobilized on water-soluble 6-O-carboxymethyl(CM)-NAPGA by Gly-Phe-Leu-Glyspacer groups (CM-NAPGA/Gly-Phe-Leu-Gly/DXR conjugate). The conjugate showed cathepsin B susceptible DXR release behavior and exhibited remarkable survival effects in mice bearing MH134Y hepatoma implanted by subcutaneous (s.c.) implantation/intravenous (i.v.) injection, compared with free DXR and CM-NAPGA-immobilized DXRs with pentamethylene spacer groups (CM-NAPGA/C5/DXR conjugate).
Details
- Language :
- English
- ISSN :
- 08839115 and 15308030
- Volume :
- 13
- Issue :
- 4
- Database :
- Supplemental Index
- Journal :
- Journal of Bioactive and Compatible Polymers
- Publication Type :
- Periodical
- Accession number :
- ejs47705794
- Full Text :
- https://doi.org/10.1177/088391159801300402