Gantrez® AN as a new polymer for the preparation of ligand-nanoparticle conjugates

被引:110
作者
Arbós, P
Wirth, M
Arangoa, MA
Gabor, F
Irache, JM
机构
[1] Univ Navarra, Ctr Galenico, Navarra 31080, Spain
[2] Univ Vienna, Inst Pharmaceut Technol & Biopharmacuet, A-1090 Vienna, Austria
关键词
Gantrez (R) AN; nanoparticles; conjugates; lectin; Sambucus nigra agglutinin; Caco-2; monolayers;
D O I
10.1016/S0168-3659(02)00015-9
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The aim of this study was to evaluate the feasibility and in vitro activity of ligand-conjugates based on the use of poly(methyl vinyl ether-co-maleic anhydride) (PVM/MA or Gantrez(R) AN). Fluorescently labelled PVM/MA nanoparticles were prepared by desolvation and cross-linkage with 1,3-diaminopropane (DP). Conjugates were obtained by incubation between the carriers and Sambucus nigra agglutinin (SNA) for I h in an aqueous medium. The lectin binding to the surface of nanoparticles was increased by both increasing the bulk ligand concentration and decreasing the amount of cross-linker. However, a concentration of about 0.3-0.4 mug DP per mg polymer was necessary to obtain maximum agglutination activity. Under optimal conditions, the amount of fixed ligand was 46 mug/mg nanoparticle (binding efficiency of 86%); although the activity of SNA conjugates was 13.3 mug/mg particle. The activity of nanoparticles, measured by the association to Caco-2 monolayers, was higher when SNA was covalently bound onto their surface. The lectin-conjugate interaction was 6-fold higher than conventional nanoparticles. Moreover, energy-dependent mechanisms were only observed in SNA-PVM/MA particles. Finally, the decrease in association in the presence of lactose demonstrates that both SNA- and SNA-conjugate-binding was due to a true lectin-sugar interaction. (C) 2002 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:321 / 330
页数:10
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