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Journal of Drug Delivery
Volume 2012, Article ID 986265, 9 pages
http://dx.doi.org/10.1155/2012/986265
Research Article

Formulation Strategies, Characterization, and In Vitro Evaluation of Lecithin-Based Nanoparticles for siRNA Delivery

1Department of Pharmaceutical Technology, Faculty of Pharmacy and Biochemistry, University of Buenos Aires, Junín 954 1113AAD Buenos Aires, Argentina
2Institute of Biochemistry and Biophysics (IQUIFIB), National Science Research Council (CONICET), Junín 954 1113AAD Buenos Aires, Argentina

Received 14 October 2011; Revised 22 December 2011; Accepted 16 January 2012

Academic Editor: Fabiana Quaglia

Copyright © 2012 Sebastián Ezequiel Pérez et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

The aim of the present work was to take advantage of lecithin’s biocompatibility along with its physicochemical properties for the preparation of lecithin-based nanocarriers for small interfering RNA (siRNA) delivery. Water lecithin dispersions were prepared in different conditions, loaded with siRNA at different N/P ratios, and evaluated for loading capacity. The most appropriate ones were then assayed for cytotoxicity and characterized in terms of particle size distribution, zeta potential, and morphology. Results demonstrated that formulations prepared at pH 5.0 and 7.0 were able to load siRNA at broad N/P ratios, and cellular uptake assays showed an efficient delivery of oligos in MCF-7 human breast cancer cells; fluorescent-labeled dsRNA mainly located next to its target, near the nucleus of the cells. No signs of toxicity were observed for broad compositions of lecithin. The physicochemical characterization of the siRNA-loaded dispersions exhibited particles of nanometric sizes and pH-dependant shapes, which make them suitable for ex vivo and in vivo further evaluation.