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Enhanced percutaneous permeability of diclofenac using a new U-type dilutable microemulsion
Marina Shevachman1, Nissim Garti, Arnon Shani
1Department of Chemistry, Faculty of Natural Sciences, Ben Gurion University of the Negev, Beer Sheva, Israel.
Drug Development and Industrial Pharmacy
|April 11, 2008
Summary
This study shows U-type microemulsions significantly enhance diclofenac sodium transdermal absorption. Jojoba oil, however, hinders drug penetration due to its structure.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Diclofenac sodium is a widely used non-steroidal anti-inflammatory drug.
- Transdermal drug delivery offers advantages over oral administration.
- Microemulsions can improve drug solubility and skin penetration.
Purpose of the Study:
- To investigate the transdermal delivery of diclofenac sodium using U-type microemulsions.
- To evaluate the effect of different oil phases on drug penetration and absorption.
- To understand the structural characteristics of microemulsions influencing drug delivery.
Main Methods:
- Formulation of a four-component U-type microemulsion system with diclofenac sodium.
- Characterization of microemulsion structure using viscosity and small angle X-ray scattering.
- Assessment of drug diffusion and distribution using Self-diffusion Nuclear Magnetic Resonance (NMR) studies.
- In vivo and in vitro evaluation of transdermal penetration and absorption in rats.
Main Results:
- Microemulsions with paraffin oil or isopropyl myristate significantly increased diclofenac sodium's in vivo transdermal penetration (two orders of magnitude) and plasma levels (one order of magnitude).
- Bicontinuous structures were observed in microemulsions with specific water fractions.
- Jojoba oil as the oil phase significantly reduced drug penetration, likely due to its molecular structure hindering diffusion.
Conclusions:
- U-type microemulsions are effective vehicles for enhancing diclofenac sodium transdermal delivery.
- The choice of oil phase critically influences drug penetration, with jojoba oil showing inhibitory effects.
- Further research is needed to optimize in vitro-in vivo correlations for transdermal studies.
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