Production and in vitro evaluation of gelatin microspheres containing an antitumour tetra-amidine.
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 microns 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.
Nastruzzi
C
C
Department of Pharmaceutical Science, University of Ferrara, Italy.
Pastesini
C
C
Cortesi
R
R
Esposito
E
E
Gambari
R
R
Menegatti
E
E
D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D001550:Benzamidines / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical; D003432:Cross-Linking Reagents / Q000737:chemistry; D004355:Drug Stability; D005780:Gelatin / Q000737:chemistry*; D005976:Glutaral / Q000737:chemistry; D006801:Humans; D007938:Leukemia / Q000378:metabolism; D008863:Microspheres; D012995:Solubility
D000970:Antineoplastic Agents; D001550:Benzamidines; D003432:Cross-Linking Reagents; D005780:Gelatin; C057886:4,4'-(2,2-bis((4-(aminoiminomethyl)-2-bromophenoxy)methyl)-1,3-propanediyl)bis(oxy))bis(3-bromobenzenecarboximidamide; D005976:Glutaral