Colon-specific 9-aminocamptothecin-HPMA copolymer conjugates containing a 1,6-elimination spacer
| Autor: | Jindřich Kopeček, Song Qi Gao, Zheng-Rong Lu, Pavla Kopečková, Boris Petri |
|---|---|
| Rok vydání: | 2006 |
| Předmět: |
Male
Colon Pharmaceutical Science Buffers Rats Sprague-Dawley chemistry.chemical_compound Drug Delivery Systems Intestine Small Polymer chemistry Copolymer Animals Methacrylamide Intestine Large Intestinal Mucosa Chromatography High Pressure Liquid Bond cleavage chemistry.chemical_classification Chemistry Polymer Rats Spectrometry Fluorescence Drug delivery Methacrylates Liberation Camptothecin Indicators and Reagents Aminocamptothecin Conjugate |
| Zdroj: | Journal of Controlled Release. 110:323-331 |
| ISSN: | 0168-3659 |
| Popis: | N-(2-Hydroxypropyl)methacrylamide (HPMA) copolymer–9-aminocamptothecin (9-AC) conjugate for oral colon-specific drug delivery was designed, synthesized, and characterized. The drug, 9-AC, was attached to the polymer carrier via a spacer containing a combination of an aromatic azo bond and a 4-aminobenzylcarbamate group. The design of the spacer ensured a fast and highly efficient release of unmodified 9-AC from the polymer in the colon by azo bond cleavage followed by a 1,6-elimination mechanism. An in vitro degradation study indicated that this conjugate was stable in simulated upper GI tract conditions, including small intestine (SI) contents, SI mucosa suspension, and in PBS (pH 1.5 and 7.4). A fast release of the unmodified drug (85 ± 10% of 9-AC in 12 h) was detected in rat cecal contents. This drug delivery system has potential in the treatment of colon cancer. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect