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Microemulsion Formulations for the Transdermal Delivery of Lapachol

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Abstract

This project was carried out to investigate the feasibility of using microemulsions for transdermal delivery of lapachol. From the screening of surfactants and oils, a range of microemulsions were developed using oleic acid, a mixture of Cremophor EL and Tween 20 and water. The solubility of lapachol was determined in these ingredients and in the formulated microemulsions. The microemulsions were characterised using cross-polarising light microscopy, their electrical conductivity, pH, zeta potential and rheology were analysed, and they were also investigated using small-angle X-ray scattering and differential scanning calorimetry. Ex vivo studies were performed using porcine ear skin and Franz diffusion cells to investigate the permeation and retention of lapachol. Systems containing different concentrations of Cremophor EL (8.4–41.6%), Tween 20 (5.4–41.6%) and oleic acid (12–31.9%) are able to form microemulsions. Lapachol was delivered more effectively through the skin from all of the microemulsions tested than by the control (oleic acid). These studies indicated that microemulsions incorporating lapachol were formed successfully and that these enhanced drug delivery and retention in the skin. Microemulsion systems may, therefore, provide promising vehicles for percutaneous delivery of lapachol.

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Abbreviations

DSC:

Differential scanning calorimetry

HLB:

Hydrophilic-lipophilic balance

HPLC:

High-performance liquid chromatography

PEG 400:

Polyethylene glycol-400

SAXS:

Small-angle X-ray scattering

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Acknowledgements

The authors thank the Laboratório Nacional de Luz Síncroton (LNLS, Campinas SP, Brazil). LNLS is acknowledged through the projects D11A-SAXS1-14558. We especially thank SAXS staff for the support. The authors also thank FECDA/NUDFAC for financial support.

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Authors and Affiliations

  1. Department of Pharmaceutical Science, Universidade Federal de Pernambuco, Avenida Professor Artur de Sá, s/n, Cidade Universitária, Recife, CEP 50740-521, Brazil

    Maria Alice Maciel Tabosa, Ana Rosa Brissant de Andrade, Davi Pereira de Santana & Leila Bastos Leal

  2. Department of Physiology, Universidade Federal de Sergipe, Cidade Universitária Professor Aloísio de Campos, Avenida Marechal Rondon s/n, Jardim Rosa Elze, São Cristóvão, CEP 49100-000, Brazil

    Ana Amélia Moreira Lira

  3. Department of Chemistry, Universidade Federal de Sergipe, Avenida Vereador Olímpio Grande, S/N, Campus Prof. Alberto Carvalho, Itabaiana, CEP 49500-000, Brazil

    Victor Hugo Vitorino Sarmento

Authors
  1. Maria Alice Maciel Tabosa
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  2. Ana Rosa Brissant de Andrade
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  3. Ana Amélia Moreira Lira
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  4. Victor Hugo Vitorino Sarmento
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  6. Leila Bastos Leal
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Correspondence to Leila Bastos Leal.

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Tabosa, M.A.M., de Andrade, A.R.B., Lira, A.A.M. et al. Microemulsion Formulations for the Transdermal Delivery of Lapachol. AAPS PharmSciTech 19, 1837–1846 (2018). https://doi.org/10.1208/s12249-018-0995-2

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