Abstract

Nanoemulsions are particularly suitable as a platform in the development of delivery systems. The type of nanoemulsion with a higher stability will offer an advantage in the preparation of a delivery system for lipophilic drugs. Nanoemulsions can be fabricated by different processing methods, which are usually categorized as either high- or low-energy methods. In this study, a comparison between two methods of preparing magnetic oil-in-water (O/W) nanoemulsions is described. The nanoemulsions were formed by sonication (the high-energy method) or by spontaneous emulsification (the low-energy method). In both cases, the oil phase was olive oil, and a phospholipid and a pegylated phospholipid were used as emulsifiers. To favor the comparison, the amounts of the components were the same in both kinds of nanoemulsions. Moreover, nanoemulsions were loaded with hydrophobic superparamagnetic nanoparticles and indomethacin. In vitro, releases studies indicated a short drug burst period followed by a prolonged phase of dissolutive drug release. The Korsmeyer-Peppas model can fit the associated kinetics. The results showed that such nanoemulsions are suitable as a platform in the development of delivering systems for lipophilic drugs. The long-term stability was also examined at different temperatures, as well as the interaction with plasma proteins. Nanoemulsion obtained by the low-energy method showed a great stability at 4 °C and at ambient temperature. Its size and polydispersity did not change over more than two months. The spontaneous emulsification method therefore has great potential for forming nanoemulsion-based delivery systems.

Highlights

  • Nanoemulsions can be recognized and defined as emulsions consisting of nanoscaled oil or water droplets dispersed in the external phase of opposite polarity by the effect of surfactant arranging at the oil/water interface [1,2]

  • The results showed that such nanoemulsions are suitable as a platform in the development of delivering systems for lipophilic drugs

  • Hydrophobic magnetic nanoparticles can be incorporated into the oil droplets of O/W nanoemulsions generating a magnetic nanoemulsion

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Summary

Introduction

Nanoemulsions can be recognized and defined as emulsions consisting of nanoscaled oil or water droplets (typically in the range 20–200 nm) dispersed in the external phase of opposite polarity by the effect of surfactant arranging at the oil/water interface [1,2]. To obtain more information about the stability of the LE nanoemulsion, we studied the samples kept at 4 ◦C and ambient temperature for a minimum of two months In both cases, the size was approximately 200 nm, and the polydispersity index never exceeded 0.13. Neither size nor polydispersity index underwent significant changes in comparison with undiluted samples This observation has important consequences for the practical application of this kind of nanoemulsion, since it can be stored in undiluted and in diluted forms. Since the adsorbed proteins control the interaction with cell membranes and the mechanism of cellular uptake, a potential future research direction should be the study of the interaction of the nanoemulsion with the biological milieu, including parameters as cytotoxicity, body distribution, and endocytosis into specific cells

Materials
Preparation of Nanoemulsions
Particle Size Measurements
Magnetic Measurements
Thermogravimetric Measurements
Lipid Determination
Iron Determination
IND Determination
In Vitro Release Assay
4.2.10. Modelling of Release Kinetics
4.2.11. Long-Term Stability Test
4.2.12. Interaction with Proteins
Findings
4.2.13. SDS-PAGE Electrophoresis
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