Association with amino acids does not enhance efficacy of polymerized liposomes as a system for lung gene delivery

ELGA BERNARDO BANDEIRA DE MELO, MIQUÉIAS LOPES-PACHECO, DÉBORA FERREIRA, TATIANA MARÓN-GUTIÉRREZ, HUGO C CASTRO-FARIA-NETO, PATRICIA RIEKEN MACEDO ROCCO, MARCELO MARCOS MORALES; NADIA CHIARAMONI, MARIA JULIETA FERNANDEZ-RUOCCO, MARIA JIMENA PRIETO, RAMIRO M PERROTA, SILVIA DEL VALLE ALONSO

Frontiers in Physiology

Frontiers Research Foundation

Lugar: Lausanne : Frontiers Research Foundation; Año: 2016 vol. 7 p. 1 - 9

Development of improved drug and gene delivery systems directly into the lungs ishighly desirable given the important burden of respiratory diseases. We aimed toevaluate the safety and efficacy of liposomes composed of photopolymerized lipids[1,2-bis-(tricosa-10,12-diynoyl)-sn-glycero-3-phosphocholine] associated with aminoacids as vectors for gene delivery into the lungs of healthy animals. Lipopolymer vesicles,in particular, are more stable than other types of liposomes. In this study, lipopolymerswere associated with L-arginine, L-tryptophan, or L-cysteine. We hypothesized that theaddition of these amino acids would enhance the efficacy of gene delivery to the lungs bythe lipopolymers. L-Arginine showed the highest association efficiency due to its positivecharge and better surface interactions. None of the formulations caused inflammation oraltered lung mechanics, suggesting that these lipopolymers can be safely administeredas aerosols. All formulations were able to induce eGFP mRNA expression in lung tissue,but the addition of amino acids reduced delivery efficacy when compared with the simplelipopolymer particle. These results indicate that this system could be further explored forgene or drug delivery targeting lung diseases.Keywords: lung, gene delivery, mechanic parameters, nanoparticles, inflammation