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The Effect of Composition and Gastric Conditions on the Self-Emulsification Process of Ibuprofen-Loaded Self-Emulsifying Drug Delivery Systems: A Microscopic and Dynamic Gastric Model Study

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ABSTRACT

Purpose

To investigate the physical processes involved in the emulsification of self-emulsifying drug delivery systems (SEDDSs) and the use of the Dynamic Gastric Model (DGM) as a characterisation tool.

Methods

SEDDSs based on soybean oil, Tween 80, Span 80 and ibuprofen were prepared and their equilibrium phase diagrams established. The emulsification behaviour in a range of media was studied using polarised light microscopy and particle sizing. The behaviour of the SEDDSs in the DGM and conventional testing equipment was assessed.

Results

A range of liquid crystalline mesophases was observed, enhanced in the presence of the drug. Polarised light microscopy showed different emulsification processes in the presence and absence of the drug, which was also manifest in different droplet sizes. The droplet size distribution varied between the DGM and the USP II dissolution apparatus.

Conclusions

The model SEDDS displays complex liquid crystalline behaviour which may be intimately involved in the emulsification process, which in turn may alter particle size on emulsification, although there remains a question as to the in vivo significance of this effect. Furthermore, we demonstrate that the DGM represents a very promising new method of assessing the biological fate of SEDDSs.

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Abbreviations

AGJwp :

artificial gastric juice without pepsin

DGM:

dynamic gastric model

HCl:

hydrochloric acid

SEDDS:

self-emulsifying drug delivery systems

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ACKNOWLEDGMENTS

The authors would like to thank the University of East Anglia for the financial support of A. M. and the University of Messina for the Erasmus placement of A. P. Access to the droplet sizer was kindly provided by the Institute of Food Research (Norwich). The authors are also grateful to Dr. Mary Parker from the Institute of Food Research for assistance with the microscopy images taken with the Olympus BX60.

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Authors and Affiliations

  1. School of Pharmacy, University of East Anglia, Norwich, NR4 7TJ, UK

    Annalisa Mercuri, Duncan Q. M. Craig & Susan A. Barker

  2. Institute of Food Research, Norwich Research Park, Colney, Norwich, NR4 7UA, UK

    Antonio Passalacqua, Martin S. J. Wickham & Richard M. Faulks

Authors
  1. Annalisa Mercuri
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  2. Antonio Passalacqua
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  3. Martin S. J. Wickham
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  5. Duncan Q. M. Craig
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  6. Susan A. Barker
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Correspondence to Susan A. Barker.

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Mercuri, A., Passalacqua, A., Wickham, M.S.J. et al. The Effect of Composition and Gastric Conditions on the Self-Emulsification Process of Ibuprofen-Loaded Self-Emulsifying Drug Delivery Systems: A Microscopic and Dynamic Gastric Model Study. Pharm Res 28, 1540–1551 (2011). https://doi.org/10.1007/s11095-011-0387-8

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