ORIGINAL ARTICLES   

Minerva Biotecnologica 2007 March;19(1):33-42

Copyright © 2007 EDIZIONI MINERVA MEDICA

language: English

Oligonucleotide transport and cellular uptake by positively charged microparticles

Mazzitelli S. ¹, Balestra C. ¹, Cortesi R. ², Esposito E. ², Nastruzzi C. ¹

¹ Department of Drug Chemistry and Technology University ofi Perugia, Perugia, Italy 2 Department of Pharmaceutical Sciences University of Ferrara, Ferrara, Italy

The production and characterization of cationic microparticles based on a methacrylate copolymer constituted of acrylic and methacrylic acid esters (Eudragit RS) and the cationic agent dioctadecyl-dimethyl-ammonium bromide (DDAB18) for the delivery of nucleic acids is described. It was found that morphological and dimensional characteristics of microparticles were influenced by some experimental parameters such as stirring speed, emulsifying agent and type of rotor. The deoxyribonucleotide Defibrotide (DFT) was associated to positively charged microparticles and its in vitro release kinetics from microparticles was determined. A study on the in vitro toxicity of cationic microparticles on cultured human cell line K562 was also performed which demonstrated that the cationic surfactant dioctadecyl-dimethyl-ammonium bromide (DDAB18) micro-particles display very low cytotoxicity.