Synthesis and characterization of thermosensitive copolymers for oral controlled drug delivery

被引:89
作者
Eeckman, F [1 ]
Moës, AJ [1 ]
Amighi, K [1 ]
机构
[1] Free Univ Brussels, Pharm Galen & Biopharm Lab, B-1050 Brussels, Belgium
关键词
thermosensitive polymers; poly(N-isopropylacrylamide); phase transition temperature; controlled drug delivery;
D O I
10.1016/j.eurpolymj.2003.11.010
中图分类号
O63 [高分子化学(高聚物)];
学科分类号
070305 ; 080501 ; 081704 ;
摘要
Poly(N'-isopropylacrylamide) (PNIPAAm) copolymers were synthesized in order to obtain co-polymers with a phase transition temperature slightly higher than the physiological temperature, as required by a new drug delivery concept described in a previous paper. Six hydrophilic comonomers bringing about a rise of the phase transition temperature were evaluated. The synthesized copolymers were characterized and the influence of the type and of the amount of the used comonomer on the phase transition temperature was discussed. Among the comonomers, Acrylamide (AAm), N-methyl-N-vinylacetamide (MVA), N-vinylacetamide (NVA), and N-vinyl-2-pyrrolidinone (VPL) were found to be capable to raise the phase transition temperature to a value slightly higher than 37 degreesC and to have adequate phase transition behavior. The selected four copolymers were subjected to an additional purification step that should make them fit to use as a controlling agent in drug delivery systems. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:873 / 881
页数:9
相关论文
共 29 条
[1]   TEMPERATURE-DEPENDENCE OF SWELLING OF CROSS-LINKED POLY(N,N'-ALKYL SUBSTITUTED ACRYLAMIDES) IN WATER [J].
BAE, YH ;
OKANO, T ;
KIM, SW .
JOURNAL OF POLYMER SCIENCE PART B-POLYMER PHYSICS, 1990, 28 (06) :923-936
[2]  
Brandrup J., 1999, Polymer handbook, VII
[3]  
Chee C. K., 2001, ACS SYM SER, V780, P223
[4]   Thermoassociative graft copolymers based on poly(N-isopropylacrylamide):: effect of added co-solutes on the rheological behaviour [J].
Durand, A ;
Hourdet, D .
POLYMER, 2000, 41 (02) :545-557
[5]   Evaluation of a new controlled-drug delivery concept based on the use of thermoresponsive polymers [J].
Eeckman, F ;
Moës, AJ ;
Amighi, K .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2002, 241 (01) :113-125
[6]   Effect of some physiological and non-physiological compounds on the phase transition temperature of thermoresponsive polymers intended for oral controlled-drug delivery [J].
Eeckman, F ;
Amighi, K ;
Moës, AJ .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2001, 222 (02) :259-270
[7]   Effect of moisture on polyvinylpyrrolidone in accelerated stability testing [J].
Fitzpatrick, S ;
McCabe, JF ;
Petts, CR ;
Booth, SW .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2002, 246 (1-2) :143-151
[8]   PHASE-TRANSITION OF AQUEOUS-SOLUTIONS OF POLY(N-ISOPROPYLACRYLAMIDE) AND POLY(N-ISOPROPYLMETHACRYLAMIDE) [J].
FUJISHIGE, S ;
KUBOTA, K ;
ANDO, I .
JOURNAL OF PHYSICAL CHEMISTRY, 1989, 93 (08) :3311-3313
[9]   Synthesis and properties of ionically modified polymers with LCST behavior [J].
Hahn, M ;
Gornitz, E ;
Dautzenberg, H .
MACROMOLECULES, 1998, 31 (17) :5616-5623
[10]  
Heskins M., 1968, J MACROMOL SCI CHEM, V2, P1441, DOI DOI 10.1080/10601326808051910