Structural effect of cationic amphiphiles in diacetylenic photopolymerizable membranes


Autoria(s): Facundo Temprana, C.; Duarte, Evandro Luiz; Lis Femia, A.; Alonso, Silvia del V.; Lamy, Maria Teresa Moura
Contribuinte(s)

UNIVERSIDADE DE SÃO PAULO

Data(s)

05/11/2013

05/11/2013

2012

Resumo

Liposomes have been an excellent option as drug delivery systems, since they are able of incorporating lipophobic and/or lipophilic drugs, reduce drug side effects, increase drug targeting, and control delivery. Also, in the last years, their use reached the field of gene therapy, as non-viral vectors for DNA delivery. As a strategy to increase system stability, the use of polymerizable phospholipids has been proposed in liposomal formulations. In this work, through differential scanning calorimetry (DSC) and electron spin resonance (ESR) of spin labels incorporated into the bilayers, we structurally characterize liposomes formed by a mixture of the polymerizable lipid diacetylenic phosphatidylcholine 1,2-bis(10,12-tricosadiynoyl)-sn-glycero-3-phosphocholine (DC8,9PC) and the zwitterionic lipid 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC), in a 1:1 molar ratio. It is shown here that the polymerization efficiency of the mixture (c.a. 60%) is much higher than that of pure DC8,9PC bilayers (c.a. 20%). Cationic amphiphiles (CA) were added, in a final molar ratio of 1:1:0.2 (DC8,9PC:DMPC:CA), to make the liposomes possible carriers for genetic material, due to their electrostatic interaction with negatively charged DNA. Three amphiphiles were tested, 1,2-dioleoyl-3-trimetylammonium-propane (DOTAP), stearylamine (SA) and trimetyl (2-miristoyloxietyl) ammonium chloride (MCL), and the systems were studied before and after UV irradiation. Interestingly, the presence of the cationic amphiphiles increased liposomes polymerization. MCL displaying the strongest effect. Considering the different structural effects the three cationic amphiphiles cause in DC8,9PC bilayers, there seem to be a correlation between the degree of DC8,9PC polymerization and the packing of the membrane at the temperature it is irradiated (gel phase). Moreover, at higher temperatures, in the bilayer fluid phase, more polymerized membranes are significantly more rigid. Considering that the structure and stability of liposomes at different temperatures can be crucial for DNA binding and delivery, we expect the study presented here contributes to the production of new carrier systems with potential applications in gene therapy. (C) 2012 Elsevier Ireland Ltd. All rights reserved.

USP

USP

FAPESP

FAPESP

CNPq

CNPq

UNQ

UNQ

CONICET

CONICET

MINCyT

MINCyT

Identificador

CHEMISTRY AND PHYSICS OF LIPIDS, CLARE, v. 165, n. 5, supl. 1, Part 2, pp. 589-600, JUL, 2012

0009-3084

http://www.producao.usp.br/handle/BDPI/41488

10.1016/j.chemphyslip.2012.06.007

http://dx.doi.org/10.1016/j.chemphyslip.2012.06.007

Idioma(s)

eng

Publicador

ELSEVIER IRELAND LTD

CLARE

Relação

CHEMISTRY AND PHYSICS OF LIPIDS

Direitos

closedAccess

Copyright ELSEVIER IRELAND LTD

Palavras-Chave #POLYMERIC LIPOSOME #ESR #SPIN LABEL #DSC #DIACETYLENIC LIPID #CATIONIC AMPHIPHILE #DRUG-DELIVERY SYSTEMS #GENE DELIVERY #LIPOSOMES #PHOSPHOLIPIDS #STABILITY #BILAYERS #CARRIERS #DNA #PRETRANSITION #POLYPLEXES #BIOCHEMISTRY & MOLECULAR BIOLOGY #BIOPHYSICS
Tipo

article

original article

publishedVersion