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
  • [1] ANTONI G, 1979, PHARM TOXICOLOGICAL, V34, P146
  • [2] Permeation enhancing polymers in oral delivery of hydrophilic macromolecules:: thiomer/GSH systems
    Bernkop-Schnürch, A
    Kast, CE
    Guggi, D
    [J]. JOURNAL OF CONTROLLED RELEASE, 2003, 93 (02) : 95 - 103
  • [3] Synthesis and characterisation of mucoadhesive thiolated polymers
    Bernkop-Schnürch, A
    Steininger, S
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2000, 194 (02) : 239 - 247
  • [4] Thiolated polymers:: synthesis and in vitro evaluation of polymer-cysteamine conjugates
    Bernkop-Schnürch, A
    Clausen, AE
    Hnatyszyn, M
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2001, 226 (1-2) : 185 - 194
  • [5] Improvement in the mucoadhesive properties of alginate by the covalent attachment of cysteine
    Bernkop-Schnürch, A
    Kast, CE
    Richter, MF
    [J]. JOURNAL OF CONTROLLED RELEASE, 2001, 71 (03) : 277 - 285
  • [6] Bernkop-Schnürch A, 2000, J PHARM SCI-US, V89, P901, DOI 10.1002/1520-6017(200007)89:7<901::AID-JPS7>3.0.CO
  • [7] 2-0
  • [8] Influence of different parameters on drug release from hydrogel systems to a biomembrane model. Evaluation by differential scanning calorimetry technique
    Castelli, F
    Pitarresi, G
    Giammona, G
    [J]. BIOMATERIALS, 2000, 21 (08) : 821 - 833
  • [9] Development of a novel nasal nicotine formulation comprising an optimal pulsatile and sustained plasma nicotine profile for smoking cessation
    Cheng, YH
    Watts, P
    Hinchcliffe, M
    Hotchkiss, R
    Nankervis, R
    Faraj, NF
    Smith, A
    Davis, SS
    Illum, L
    [J]. JOURNAL OF CONTROLLED RELEASE, 2002, 79 (1-3) : 243 - 254
  • [10] FONTANA A, 1974, CHEM THIOL 1, P288