Preparation, Characterization and In Vivo Evaluation of Nanoemulsions for The Controlled Delivery of The Antiobesity Agent N-Oleoylethanolamine

Abstract

>Aims:N-oleoylethanolamine (OEA) is a lipid mediator that acts as a satiety factor. The main limiting factor for its administration is its poor water solubility. We designed and characterized new nanoemulsions as delivery system for hydrophobic compounds such as OEA. Materials & methods: The nanoemulsion components and preparation methods were selected in order to achieve the desired final properties. Then, we evaluated the in vivo properties of the nanoemulsions as drug-delivery systems testing the anorectic effects of OEA in rats after both intragastric and intraperitoneal administration. The in vivo toxicity of the nanoemulsions was evaluated after a 3-week treatment. Results: Nanoemulsions proved to be stable, nontoxic and had no effect on feeding behavior when administered without OEA. The effects of OEA were observable after its oral and parenteral administration with the nanoemulsions to 24-h fasted rats, finding a better efficacy compared with a vehicle containing Tween^® 20 (Sigma-Aldrich, MO, USA) after oral administration. Conclusion: These results support the efficacy of these nanoemulsions to deliver highly hydrophobic bioactive drugs.

Original submitted 2 October 2013; Revised submitted 3 February 2014

Keywords::

• drug delivery
• food intake
• nanoemulsion
• OEA
• parenteral emulsion
• poloxamer P188

Financial & competing interests disclosure

This work was supported by grants number MAT2010-20370 and MAT2010-15101 from Fondo Europeo de Desarrollo Regional funds and Ministry of Education and Sciences; grants P07-FQM-03099 and P11-FQM-7074 from the Andalusian Ministry of Economy, Innovation and Science; grants RD06/0001/0000 and RD012/0028/0001 of the Red de Trastornos Adictivos Temáticas de Investigación Cooperativa en Salud network from the Spanish Health Institute Carlos III; and grant number TV3 386/C/2011 from Fundació La Telemarató. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.

Ethical conduct of research

The authors state that they have obtained appropriate institutional review board approval or have followed the principles outlined in the Declaration of Helsinki for all human or animal experimental investigations. In addition, for investigations involving human subjects, informed consent has been obtained from the participants involved.

Additional information

Funding

This work was supported by grants number MAT2010-20370 and MAT2010-15101 from Fondo Europeo de Desarrollo Regional funds and Ministry of Education and Sciences; grants P07-FQM-03099 and P11-FQM-7074 from the Andalusian Ministry of Economy, Innovation and Science; grants RD06/0001/0000 and RD012/0028/0001 of the Red de Trastornos Adictivos Temáticas de Investigación Cooperativa en Salud network from the Spanish Health Institute Carlos III; and grant number TV3 386/C/2011 from Fundació La Telemarató. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.