Journal
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
Volume 83, Issue 3, Pages 358-363Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejpb.2012.10.012
Keywords
Gene delivery; Cationic lipids; Polyethylenimine; Interleukin 12 (IL-12); Folate receptors
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Funding
- University of Navarra Foundation (FUN)
- Caja de Ahorros de Navarra (CAN)
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In this work, we have developed and evaluated a new targeted lipopolyplex (LPP), by combining polyethylenimine (PEI), 1,2-dioleoy1-3-(trimethylammonium) propane (DOTAP)/Chol liposomes, the plasmids pCMVLuc/pCMVIL-12, and the ligand folic acid (FA), able to transfect HeLa and B16-F10 cells in the presence of very high concentration of serum (60% FBS). These complexes (Fol-LPP) have a net positive surface charge. The combination of folic acid with lipopolyplexes also enhanced significantly the transfection activity of the therapeutic gene interleukin-12 (IL-12), without any significant cytotoxicity. The specificity of the folate receptor (FR)-mediated gene transfer was corroborated by employing a folate receptor deficient cell line (HepG2). This formulation improved gene delivery showed by conventional lipoplexes or polyplexes resulting an efficient, simple, and nontoxic method for gene delivery of therapeutic genes in vitro and very probably in vivo. (C) 2012 Elsevier B.V. All rights reserved.
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