Synthesis and characterization of thiomers of polyaspartamide type

被引：20
作者：
Bilicic, MB
Filipovic-Grcic, J
Martinac, A
Barbaric, M
Zorc, B
Cetina-Cizmek, B
Tudja, P
机构：
[1] Univ Zagreb, Fac Pharm & Biochem, Zagreb 10000, Croatia
[2] Res Inst Ltd, PLIVA, Zagreb 10000, Croatia
来源：
INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2005年 / 291卷 / 1-2期
关键词：
thiomer; polyaspartamide; thioglycolic acid; mucoadhesion; microparticles;
D O I：
10.1016/j.ijpharm.2004.07.058
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Synthesis of poly[alpha,beta-(N-2-hydroxyethyl-DL-aspartamide)]-thioglycolic acid (PHEA-TGA) conjugate as a new polyaspartamide thiomer is described. The parent polymer PHEA is chemically modified by introducing sulphydryl-bearing compound thioglycolic acid. By varying the reaction conditions several batches of PHEA-TGA conjugates were prepared and analyzed. Tensile studies revealed that total work of adhesion of PHEA-TGA increased more than twice compared to the unmodified polymer. Microparticles prepared from the thiolated polymer preserved its bioadhesive properties. (C) 2004 Elsevier B.V. All rights reserved.
引用
收藏
页码：211 / 219
页数：9
相关论文
共 23 条
[11]   Coupling of the antiviral agent zidovudine to polyaspartamide and in vitro drug release studies [J].
Giammona, G ;
Cavallaro, G ;
Fontana, G ;
Pitarresi, G ;
Carlisi, B .
JOURNAL OF CONTROLLED RELEASE, 1998, 54 (03) :321-331
[12]  
GUM JR, 1992, J BIOL CHEM, V267, P21375
[13]   In vitro evaluation of the viscoelastic properties of chitosan-thioglycolic acid conjugates [J].
Hornof, MD ;
Kast, CE ;
Bernkop-Schnürch, A .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2003, 55 (02) :185-190
[14]   Self-aggregates of poly(2-hydroxyethyl aspartamide) copolymers loaded with methotrexate by physical and chemical entrapments [J].
Kang, H ;
Kim, JD ;
Han, SH ;
Chang, IS .
JOURNAL OF CONTROLLED RELEASE, 2002, 81 (1-2) :135-144
[15]   Thiolated polymers -: thiomers:: development and in vitro evaluation of chitosan-thioglycolic acid conjugates [J].
Kast, CE ;
Bernkop-Schnürch, A .
BIOMATERIALS, 2001, 22 (17) :2345-2352
[16]   TEMPERATURE EFFECT ON MOLECULAR-WEIGHT AND OPTICAL PURITY OF ANHYDROPOLYASPARTIC ACID PREPARED BY THERMAL POLYCONDENSATION [J].
KOKUFUTA, E ;
SUZUKI, S ;
HARADA, K .
BULLETIN OF THE CHEMICAL SOCIETY OF JAPAN, 1978, 51 (05) :1555-1556
[17]   Gemfibrozil encapsulation and release from microspheres and macromolecular conjugates [J].
Martinac, A ;
Filipovic-Grcic, J ;
Barbaric, M ;
Zorc, BK ;
Voinovich, D ;
Jalsenjak, I .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2002, 17 (4-5) :207-216
[18]  
Morioka Y, 1997, BIOL PHARM BULL, V20, P825
[19]   SYNTHESIS OF ALPHA,BETA-POLY [(2-HYDROXYETHYL)-DL-ASPARTAMIDE], A NEW PLASMA EXPANDER [J].
NERI, P ;
ANTONI, G ;
BENVENUTI, F ;
COCOLA, F ;
GAZZEI, G .
JOURNAL OF MEDICINAL CHEMISTRY, 1973, 16 (08) :893-897
[20]   Macromolecular prodrugs X. Kinetics of fenoprofen release from PHEA-fenoprofen conjugate [J].
van der Merwe, T ;
Boneschans, B ;
Zorc, B ;
Breytenbach, J ;
Zovko, M .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2002, 241 (02) :223-230
123