Microemulsion Formulations for the Transdermal Delivery of Lapachol

  • Maria Alice Maciel Tabosa
  • Ana Rosa Brissant de Andrade
  • Ana Amélia Moreira Lira
  • Victor Hugo Vitorino Sarmento
  • Davi Pereira de Santana
  • Leila Bastos Leal
Research Article
  • 20 Downloads

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.

KEY WORDS

controlled release drug delivery systems in vitro models microemulsion percutaneous permeability skin 

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

Notes

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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Copyright information

© American Association of Pharmaceutical Scientists 2018

Authors and Affiliations

  • Maria Alice Maciel Tabosa
    • 1
  • Ana Rosa Brissant de Andrade
    • 1
  • Ana Amélia Moreira Lira
    • 2
  • Victor Hugo Vitorino Sarmento
    • 3
  • Davi Pereira de Santana
    • 1
  • Leila Bastos Leal
    • 1
  1. 1.Department of Pharmaceutical ScienceUniversidade Federal de PernambucoRecifeBrazil
  2. 2.Department of PhysiologyUniversidade Federal de SergipeSão CristóvãoBrazil
  3. 3.Department of ChemistryUniversidade Federal de SergipeItabaianaBrazil

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