PRODUCTION AND IN-VITRO EVALUATION OF GELATIN MICROSPHERES CONTAINING AN ANTITUMOR TETRA-AMIDINE

被引:26
作者
NASTRUZZI, C
PASTESINI, C
CORTESI, R
ESPOSITO, E
GAMBARI, R
MENEGATTI, E
机构
[1] Department of Pharmaceutical Science, University of Ferrara
[2] Biotechnology Centre, University of Ferrara
关键词
D O I
10.3109/02652049409040454
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
The preparation and characterization of gelatin microspheres (GMs) containing the antitumour aromatic tetra-amidine TAPP-Br and its release characteristics from microspheres are described. Spherical gelatin microspheres, showing a high percentage of drug encapsulation (over 95 per cent) and an average diameter of 16 mum were obtained by a coacervation. method. In addition, the effects of various reaction parameters on the production and chemical hardening of GMs have been investigated. In order to compare the TAPP-Br release profiles from GMs prepared with different procedures, in vitro studies were carried out. The biological effect of TAPP-Br released from gelatin microspheres was determined on 'in vitro' cultured tumour cell lines, showing that, after encapsulation, TAPP-Br still retains antiproliferative activity comparable with that exhibited by the free drug. Taken together, the results obtained suggest that gelatin-based microspheres offer excellent potential as carriers for the controlled release of polyamidines in anticancer chemotherapy.
引用
收藏
页码:249 / 260
页数:12
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