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Pegylated Nanocapsules Produced by an Organic Solvent-Free Method: Evaluation of their Stealth Properties

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Abstract

Purpose

To develop from an original process, a novel generation of stealth lipidic nanocapsules in order to improve the lipophilic drug delivery in accessible sites.

Materials and Methods

Nanocapsules covered by PEG1500 stearate were obtained by a low energy emulsification method. Conductivity measurements and ternary diagram were performed to describe the formulation mechanism. Hemolytic dosage CH50 and pharmacokinetic study in rats have been achieved in order to study the stealth properties of nanocapsules.

Results

Transition from an O/W emulsion to a w/O/W emulsion was necessary to produce PEG1500 stearate nanocapsules. Interestingly nanocapsules with a size around 26 nm and a polydispersity index inferior to 0.1 were obtained. The CH50 test has revealed a very weak complement consumption in the presence of such nanocapsules. Moreover, after intravenous injection into rats, PEG1500 stearate nanocapsules exhibited long circulating properties. The experimental data support the concept of steric repulsion of the surface towards proteins, displayed by nanocapsules covered with PEG1500 stearate. These in vivo results were in agreement with the PEG1500 density calculated at the nanocarrier surface.

Conclusions

Injectable drug carriers have been developed. Their long-circulating properties could confer them a strong potential for lipophilic drug targeting.

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Acknowledgments

The authors thank O. Lambert for Cryo-TEM studies (UMR-CNRS 5471, Bordeaux, F−33405 France; Université de Bordeaux 1, Bordeaux, F-33405 France). We also want to thank Andréanne Bouchard (University of Technology, Delft, NL-2600 AA The Netherlands) for her valuable comments and suggestions. This work was supported by the departmental committee of Maine-et-Loire of “Ligue contre le cancer.”

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Authors and Affiliations

  1. Inserm U646, Université d'Angers, Angers, F-49100, France

    Arnaud Béduneau, Patrick Saulnier, Nicolas Anton, François Hindré, Catherine Passirani & Jean-Pierre Benoit

  2. UMR-CNRS 6052, ENSC, Rennes, F-35700, France

    Holisoa Rajerison & Nicolas Noiret

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  1. Arnaud Béduneau
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  2. Patrick Saulnier
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Correspondence to Patrick Saulnier.

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Béduneau, A., Saulnier, P., Anton, N. et al. Pegylated Nanocapsules Produced by an Organic Solvent-Free Method: Evaluation of their Stealth Properties. Pharm Res 23, 2190–2199 (2006). https://doi.org/10.1007/s11095-006-9061-y

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  • DOI: https://doi.org/10.1007/s11095-006-9061-y

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