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Published on: December 23, 2016
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Mucus permeating thiolated self-emulsifying drug delivery systems
Julia Rohrer1, Alexandra Partenhauser1, Sabine Hauptstein1
1Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innrain 80/82, Innsbruck, Austria.
Summary
Novel thiol-conjugates were developed to enhance self-emulsifying drug delivery systems (SEDDS) for improved mucus permeation. These modified SEDDS demonstrate superior performance over conventional systems, offering a promising new carrier for lipophilic drug delivery.
Area of Science:
- Pharmaceutical Sciences
- Biomaterials Engineering
- Drug Delivery Systems
Background:
- Mucus presents a significant barrier to self-emulsifying drug delivery systems (SEDDS) intended for epithelial membrane targeting.
- Overcoming the mucus layer is crucial for enhancing the efficacy of oral drug delivery systems.
Purpose of the Study:
- To develop novel SEDDS capable of effectively penetrating the mucus barrier.
- To synthesize and characterize thiol-conjugates for improved mucus interaction and drug delivery.
Main Methods:
- Synthesis of two novel thiol-conjugates: N-dodecyl-4-mercaptobutanimidamide (TBA-D) and 2-mercapto-N-octylacetamide (TGA-O).
- Incorporation of thiol-conjugates into SEDDS formulations.
- Physicochemical characterization (e.g., droplet size, zeta potential) using dynamic light scattering.
- In vitro mucus interaction studies employing multiple particle tracking, rotational silicone tubes, and rheology.
Main Results:
- Successful synthesis and characterization of TBA-D (yield 55%) and TGA-O (yield 70%) via NMR analysis.
- Thiolated SEDDS exhibited droplet sizes around 50 nm and zeta potential near 0 mV.
- Enhanced diffusion coefficients (up to 0.871 × 10⁻⁹ cm²/s) and increased permeation through mucus were observed for thiolated SEDDS.
- Rheological studies confirmed significant mucolytic activity of the thiol-conjugates.
Conclusions:
- Low molecular weight thiol-conjugates effectively improve mucus permeation of SEDDS.
- The developed thiolated SEDDS demonstrate superior mucus penetration compared to conventional SEDDS.
- These novel SEDDS represent a promising carrier system for enhancing the delivery of lipophilic drugs.
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