International Journal of Pharmaceutics 2014-12-10

Anionic nanoparticles based on Span 80 as low-cost, simple and efficient non-viral gene-transfection systems.

A Pensado, I Fernandez-Piñeiro, B Seijo, A Sanchez

Index: Int. J. Pharm. 476(1-2) , 23-30, (2015)

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Abstract

The existing strategies in the design of non-viral vectors for gene therapy are primarily conceived for cationic systems. However, the safety concerns associated with the use of positively charged systems for nucleic acid delivery and several reports regarding the efficacy of negatively charged systems highlights the need for improved gene-delivery vectors. With these premises in mind, we investigated the development of new negatively charged nanoparticles based on Sorbitan esters (Span(®)) – extremely cheap excipients broadly used in the pharmaceutical industry – on the basis of a simple, one-step and easily scalable procedure. For their specific use in gene therapy, we have incorporated oleylamine (OA) or poly-L-arginine (PA) into these nanosystems. Thus, we used Sorbitan monooleate (Span(®) 80) to design Span(®) 80-oleylamine and Span(®) 80-poly-L-arginine nanosystems (SP-OA and SP-PA, respectively). These systems can associate with the model plasmid pEGFP-C3 and show mean particle sizes of 304 nm and 247 nm and surface charges of -13 mV and -17 mV, respectively. The nanoparticles developed were evaluated in terms of in vitro cell viability and transfection ability. Both systems exhibited an appropriate cell-toxicity profile and are able to transfect the plasmid effectively. Specifically, the nanosystems including OA among their components provided higher transfection levels than the SP-PA nanoparticles. In conclusion, anionic nanoparticles based on Span(®) 80 can be considered low-cost, simple and efficient non-viral anionic gene-transfection systems.Copyright © 2014 Elsevier B.V. All rights reserved.