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
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
    Giammona, G
    Cavallaro, G
    Fontana, G
    Pitarresi, G
    Carlisi, B
    [J]. 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
    Hornof, MD
    Kast, CE
    Bernkop-Schnürch, A
    [J]. 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
    Kang, H
    Kim, JD
    Han, SH
    Chang, IS
    [J]. JOURNAL OF CONTROLLED RELEASE, 2002, 81 (1-2) : 135 - 144
  • [15] Thiolated polymers -: thiomers:: development and in vitro evaluation of chitosan-thioglycolic acid conjugates
    Kast, CE
    Bernkop-Schnürch, A
    [J]. BIOMATERIALS, 2001, 22 (17) : 2345 - 2352
  • [16] TEMPERATURE EFFECT ON MOLECULAR-WEIGHT AND OPTICAL PURITY OF ANHYDROPOLYASPARTIC ACID PREPARED BY THERMAL POLYCONDENSATION
    KOKUFUTA, E
    SUZUKI, S
    HARADA, K
    [J]. BULLETIN OF THE CHEMICAL SOCIETY OF JAPAN, 1978, 51 (05) : 1555 - 1556
  • [17] Gemfibrozil encapsulation and release from microspheres and macromolecular conjugates
    Martinac, A
    Filipovic-Grcic, J
    Barbaric, M
    Zorc, BK
    Voinovich, D
    Jalsenjak, I
    [J]. 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
    NERI, P
    ANTONI, G
    BENVENUTI, F
    COCOLA, F
    GAZZEI, G
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1973, 16 (08) : 893 - 897
  • [20] Macromolecular prodrugs X. Kinetics of fenoprofen release from PHEA-fenoprofen conjugate
    van der Merwe, T
    Boneschans, B
    Zorc, B
    Breytenbach, J
    Zovko, M
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2002, 241 (02) : 223 - 230