کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1427733 986877 2006 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Colon-specific 9-aminocamptothecin-HPMA copolymer conjugates containing a 1,6-elimination spacer
موضوعات مرتبط
مهندسی و علوم پایه مهندسی مواد بیومتریال
پیش نمایش صفحه اول مقاله
Colon-specific 9-aminocamptothecin-HPMA copolymer conjugates containing a 1,6-elimination spacer
چکیده انگلیسی

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.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Controlled Release - Volume 110, Issue 2, 10 January 2006, Pages 323–331
نویسندگان
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