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Loading of praziquantel in the crystal lattice of solid lipid nanoparticles

Studies by DSC and SAXS

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Abstract

Praziquantel (PZQ) is the drug of choice for oral treatment of schistosomiasis and other fluke infections that affect humans. Its low oral bioavailability demands the development of innovative strategies to overcome the first pass metabolism. In this article, solid lipid nanoparticles loaded with PZQ (PZQ-SLN) were prepared by a modified oil-in-water microemulsion method selecting stearic acid as lipid phase after solubility screening studies. The mean particle size (Z-Ave) and zeta potential (ZP) were 500 nm and −34.0 mV, respectively. Morphology and shape of PZQ-SLN were analysed by scanning electron microscopy revealing the presence of spherical particles with smooth surface. Differential scanning calorimetry suggested that SLN comprised a less ordered arrangement of crystals and the drug was molecularly dispersed in the lipid matrix. No supercooled melts were detected. The entrapment efficiency (EE) and loading capacity of PZQ, determined by high performance liquid chromatography, were 99.06 ± 0.3 and 17.48 ± 0.05, respectively. Effective incorporation of PZQ into the particles was confirmed by small angle X-ray scattering revealing the presence of a lipid lamellar structure. Stability parameters of PZQ-SLN stored at room temperature (25 °C) and at 4 °C were checked by analysing Z-Ave, ZP and the EE for a period of 60 days. Results showed a relatively long-term physical stability after storage at 4 °C, without drug expulsion.

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Acknowledgements

Authors wish to thank Dr. Marcelo Ornaghi Orlandi and Tarek Fernandes for SEM analysis. Laboratorio Nacional de Luz Sincrotron (LNLS) is acknowledged and especially SAXS’ staff support. Financial support provided by FAPESP (Fundação de Amparo a Pesquisa), CNPq (Conselho Nacional de Desenvolvimento Científico e Tecnológico) and CAPES (Coordenação de Aperfeiçoamento de Pessoal de Nível Superior) for Ana Luiza R. de Souza and by FCT (Fundação para a Ciência e Tecnologia) for Tatiana Andreani under the reference SFRH/BD/60640/2009 are acknowledged. The authors also acknowledge FCT under the reference PTDC/SAU-FAR/113100/2009.

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Authors and Affiliations

  1. School of Pharmaceutical Sciences, Paulista State University, Araraquara, Brazil

    Ana Luiza Ribeiro de Souza, Adélia Emília de Almeida & Maria Palmira Daflon Gremião

  2. Department of Biology and Environment, University of Trás-os-Montes e Alto Douro, P.O. Box 1013, 5000-911, Vila Real, Portugal

    Ana Luiza Ribeiro de Souza, Tatiana Andreani & Amélia M. Silva

  3. Centre for Research and Technology of Agro-Environmental and Biological Sciences, Vila Real, Portugal

    Tatiana Andreani & Amélia M. Silva

  4. Chemistry Research Centre, Chemistry Department, University of Trás-os-Montes e Alto Douro, Vila Real, Portugal

    Fernando M. Nunes

  5. Institute of Chemistry, Paulista State University, Araraquara, Brazil

    Douglas Lopes Cassimiro & Clóvis Augusto Ribeiro

  6. Department of Chemistry, Federal University of Sergipe, Itabaiana, SE, Brazil

    Victor Hugo Vitorino Sarmento

  7. Faculty of Health Sciences, Department of Pharmaceutical Technology, Fernando Pessoa University, UFP, Rua Carlos da Maia, 296, Office S.1, P-4200-150, Porto, Portugal

    Eliana B. Souto

  8. Institute of Biotechnology and Bioengineering, Centre of Genomics and Biotechnology, University of Trás-os-Montes e Alto Douro (IBB-CGB/UTAD), Vila Real, Portugal

    Eliana B. Souto

Authors
  1. Ana Luiza Ribeiro de Souza
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  2. Tatiana Andreani
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  3. Fernando M. Nunes
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  4. Douglas Lopes Cassimiro
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  5. Adélia Emília de Almeida
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  8. Maria Palmira Daflon Gremião
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  9. Amélia M. Silva
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  10. Eliana B. Souto
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Correspondence to Eliana B. Souto.

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de Souza, A.L.R., Andreani, T., Nunes, F.M. et al. Loading of praziquantel in the crystal lattice of solid lipid nanoparticles. J Therm Anal Calorim 108, 353–360 (2012). https://doi.org/10.1007/s10973-011-1871-4

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  • DOI: https://doi.org/10.1007/s10973-011-1871-4

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