Enzymatic and anaerobic degradation of amylose based acrylic copolymers, for use as matrices for drug release

被引:17
作者
Alias, J. [1 ]
Goni, I. [1 ]
Gurruchaga, M. [1 ]
机构
[1] Univ Basque Country, Fac Quim, POLYMAT Inst Polymer Mat, Dept Ciencia & Tecnol Polimeros, San Sebastian 2080, Guipuzcoa, Spain
关键词
enzymatic degradation; in vitro fermentation; drug delivery; starch copolymers; colon delivery;
D O I
10.1016/j.polymdegradstab.2006.12.012
中图分类号
O63 [高分子化学(高聚物)];
学科分类号
070305 ; 080501 ; 081704 ;
摘要
The aim of this investigation is the use of starch for effective colon-targeted drug delivery. To this end, high-amylose starch-based copolymers were tested as matrices for drug delivery. Ethyl methacrylate (EMA) was grafted onto a high-amylose starch (A). Copolymer synthesis and characterization as well as other experiments to test the enzymatic resistance and the capacity for fermentation of these products by colonic bacteria were carried out. Finally, tablets developed with our copolymers were tested to observe the dissolution behaviour of a model drug and a model protein. Our findings indicate that large quantities of grafted PEMA are not necessary to obtain high enzymatic resistance. Fermentation experiments indicate that the carbohydrate of A-EMA copolymers is susceptible to fermentation in spite of the EMA coating around the amylose backbone and that these materials could favour colon-targeted delivery. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:658 / 666
页数:9
相关论文
共 17 条
[1]  
ALDERMAN D A, 1984, International Journal of Pharmaceutical Technology and Product Manufacture, V5, P1
[2]   Enzymatically degradable and pH-sensitive hydrogels for colon-targeted oral drug delivery. I. Synthesis and characterization [J].
Bajpai, SK ;
Saxena, S .
JOURNAL OF APPLIED POLYMER SCIENCE, 2004, 92 (06) :3630-3643
[3]   Carboxymethyl high amylose starch (CM-HAS) as excipient for Escherichia coli oral formulations [J].
Calinescu, C ;
Mulhbacher, J ;
Nadeau, T ;
Fairbrother, JM ;
Mateescu, MA .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2005, 60 (01) :53-60
[4]   Efficacy of nonfetal human RPE for photoreceptor rescue: A study in dystrophic RCS rats [J].
Castillo, BV ;
delCerro, M ;
White, RM ;
Cox, C ;
Wyatt, J ;
Nadiga, G ;
delCerro, C .
EXPERIMENTAL NEUROLOGY, 1997, 146 (01) :1-9
[5]   Ethyl methacrylate grafted on two starches as polymeric matrices for drug delivery [J].
Echeverria, I ;
Silva, I ;
Goñi, I ;
Gurruchaga, M .
JOURNAL OF APPLIED POLYMER SCIENCE, 2005, 96 (02) :523-536
[6]   Studies on α-amylase degradation of retrograded starch gels from waxy maize and high-amylopectin potato [J].
Fredriksson, H ;
Björck, I ;
Andersson, R ;
Liljeberg, H ;
Silverio, J ;
Eliasson, AC ;
Åman, P .
CARBOHYDRATE POLYMERS, 2000, 43 (01) :81-87
[7]   SYNTHESIS OF GRAFT-COPOLYMERS OF ACRYLIC-MONOMERS ON AMYLOSE - EFFECT OF REACTION-TIME [J].
GONI, I ;
GURRUCHAGA, M ;
VAZQUEZ, B ;
VALERO, M ;
GUZMAN, GM .
EUROPEAN POLYMER JOURNAL, 1992, 28 (08) :975-979
[8]   ANALYSIS OF GRAFT-COPOLYMERS ONTO STARCH BY C-13 NMR-SPECTROSCOPY [J].
GURRUCHAGA, M ;
GONI, I ;
VAZQUEZ, B ;
VALERO, M ;
GUZMAN, GM .
MACROMOLECULES, 1992, 25 (12) :3009-3014
[9]   Amylose as a coating for drug delivery to the colon: Preparation and in vitro evaluation using 5-aminosalicylic acid pellets [J].
Milojevic, S ;
Newton, JM ;
Cummings, JH ;
Gibson, GR ;
Botham, RL ;
Ring, SG ;
Stockham, M ;
Allwood, C .
JOURNAL OF CONTROLLED RELEASE, 1996, 38 (01) :75-84
[10]  
Muraoka M, 1998, Nihon Rinsho, V56, P788