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Updated: Oct 1, 2025
Preparation and Characterization of Nanoliposomes for the Entrapment of Bioactive Hydrophilic Globular Proteins
Published on: August 31, 2019
Preparation and Evaluation of Charge Reversal Solid Lipid Nanoparticles
Christoph Federer1, Helen Victoria Spleis1, Simona Summonte1
1Thiomatrix Forschungs-und Beratungs GmbH, Trientlgasse 65, 6020 Innsbruck, Austria; Center for Chemistry and Biomedicine, Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria.
This study developed novel solid lipid nanoparticles (SLN) that change charge in response to intestinal alkaline phosphatase (IAP). These IAP-triggered SLN show potential for targeted drug delivery in the intestine.
Area of Science:
- Nanotechnology
- Biochemistry
- Materials Science
Background:
- Solid lipid nanoparticles (SLN) are investigated for drug delivery.
- Targeted delivery to the intestine requires overcoming mucus barriers and interacting with specific enzymes.
- Intestinal alkaline phosphatase (IAP) is an enzyme present in the intestinal lining.
Purpose of the Study:
- To design and characterize SLN with an intestinal alkaline phosphatase (IAP)-triggered charge reversion mechanism.
- To evaluate the in vitro and ex vivo performance of these charge-reversal SLN.
Main Methods:
- Step-wise hot microemulsion method used to prepare SLN.
- SLN incorporated a monophosphate ester-bearing surfactant and a cationic surfactant.
- Characterization included particle size, PDI, zeta potential, mucin interaction, and hemolysis assays.
Main Results:
- SLN (92 nm, PDI 0.33) remained stable for one year.
- IAP triggered charge reversion from -18.4 mV to +16.5 mV, with 82% phosphate cleavage.
- Enhanced mucin interaction and cell membrane interaction (85% hemolysis) observed with IAP treatment.
Conclusions:
- Charge-reversal SLN demonstrate enzyme-triggered surface modification.
- These SLN show enhanced interaction with intestinal mucus and cell membranes in the presence of IAP.
- The developed SLN hold promise as drug delivery systems for enzyme-rich environments like the intestine.
