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Solid Lipid Nanoparticles as Delivery Systems for Bromocriptine

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Abstract

Purpose

The present investigation describes a formulative study for the development of innovative drug delivery systems for bromocriptine.

Methods

Solid lipid nanoparticles (SLN) based on different lipidic components have been produced and characterized. Morphology and dimensional distribution have been investigated by electron microscopy and Photon Correlation Spectroscopy. The antiparkinsonian activities of free bromocriptine and bromocriptine encapsulated in nanostructured lipid carriers were evaluated in 6-hydroxydopamine hemilesioned rats, a model of Parkinson’s disease.

Results

Tristearin/tricaprin mixture resulted in nanostructured lipid carriers with stable mean diameter up to 6 months from production. Bromocriptine was encapsulated with high entrapment efficiency in all of the SLN samples, particularly in the case of tristearin/tricaprin mixture. Bromocriptine encapsulation did not change nanoparticle dimensions. In vitro release kinetics based on a dialysis method demonstrated that bromocriptine was released in a prolonged fashion for 48 h. Tristearin/tricaprin nanoparticles better controlled bromocriptine release. Both free and encapsulated bromocriptine reduced the time spent on the blocks (i.e. attenuated akinesia) in the bar test, although the action of encapsulated bromocriptine was more rapid in onset and prolonged.

Conclusions

It can be concluded that nanostructured lipid carriers encapsulation may represent an effective strategy to prolong the half-life of bromocriptine.

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Acknowledgements

Authors are grateful to Dr. Fabrizio Bortolotti (University of Ferrara) for HPLC technical assistance. This work was supported by Regione Emilia Romagna, Spinner Project.

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Authors and Affiliations

  1. Department of Pharmaceutical Sciences, University of Ferrara, 44100, Ferrara, Italy

    Elisabetta Esposito, Elisa Sivieri, Francesco Lain, Enea Menegatti & Rita Cortesi

  2. Department of Experimental and Clinical Medicine, Section of Pharmacology, and Istituto Nazionale di Neuroscienze, University of Ferrara, 44100, Ferrara, Italy

    Martina Fantin, Matteo Marti & Michele Morari

  3. Macromolecular Chemistry II, University of Bayreuth, Bayreuth, Germany

    Markus Drechsler

  4. Department of Science Applied to Complex Systems and CNISM, Università Politecnica delle Marche, Ancona, Italy

    Lydia Paccamiccio & Paolo Mariani

  5. Dipartimento di Scienze Farmaceutiche, Via Fossato di Mortara, 19, 44100, Ferrara, Italy

    Elisabetta Esposito

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Correspondence to Elisabetta Esposito.

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Esposito, E., Fantin, M., Marti, M. et al. Solid Lipid Nanoparticles as Delivery Systems for Bromocriptine. Pharm Res 25, 1521–1530 (2008). https://doi.org/10.1007/s11095-007-9514-y

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