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Poly(Lactide-co-Glycolide) Nanocapsules Containing Benzocaine: Influence of the Composition of the Oily Nucleus on Physico-Chemical Properties and Anesthetic Activity

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ABSTRACT

Purpose

The aim of this work was to investigate the influence of the oily nucleus composition on physico-chemical properties and anesthetic activity of poly (lactide-co-glycolide) nanocapsules with benzocaine.

Methods

Nanocapsules containing benzocaine were prepared with three different oily nucleus composition and characterized by mean diameter, polydispersivity, zeta potential, pH and stability were investigated as a function of time. In vitro release kinetics were performed in a system with two compartments separated by a cellulose membrane. Intensity and duration of analgesia were evaluated in rats by sciatic nerve blockade.

Results

The greatest stability, slower release profile and improvement in the local anesthetic activity of BZC were obtained with the formulation using USP mineral oil as component.

Conclusions

Results from our study provide useful perspectives on selection of the primary materials needed to produce suspensions of polymeric nanocapsules able to act as carriers of BZC, with potential future application in the treatment of pain.

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ACKNOWLEDGMENTS

The authors thank FAPESP (processes 06-00121-9 and 07/00127-0), CNPq and Fundunesp for financial support.

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Authors and Affiliations

  1. Department of Environmental Engineering, São Paulo State University (UNESP), Av. Três de Março, 511, Sorocaba, SP, 18087–180, Brazil

    Nathalie Ferreira Silva de Melo, Renato Grillo, André Henrique Rosa & Leonardo Fernandes Fraceto

  2. Department of Biochemistry, State University of Campinas (UNICAMP), 13083–970, Campinas, SP, Brazil

    Nathalie Ferreira Silva de Melo, Renato Grillo, Viviane Aparecida Guilherme, Daniele Ribeiro de Araujo, Eneida de Paula & Leonardo Fernandes Fraceto

  3. Human and Natural Sciences Center, Federal University of ABC (UFABC), 09210–170, Santo André, SP, Brazil

    Daniele Ribeiro de Araujo

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  1. Nathalie Ferreira Silva de Melo
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  2. Renato Grillo
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  3. Viviane Aparecida Guilherme
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  4. Daniele Ribeiro de Araujo
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  5. Eneida de Paula
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  7. Leonardo Fernandes Fraceto
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Correspondence to Leonardo Fernandes Fraceto.

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de Melo, N.F.S., Grillo, R., Guilherme, V.A. et al. Poly(Lactide-co-Glycolide) Nanocapsules Containing Benzocaine: Influence of the Composition of the Oily Nucleus on Physico-Chemical Properties and Anesthetic Activity. Pharm Res 28, 1984–1994 (2011). https://doi.org/10.1007/s11095-011-0425-6

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  • DOI: https://doi.org/10.1007/s11095-011-0425-6

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