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Melatonin-loaded lecithin/chitosan nanoparticles: physicochemical characterisation and permeability through Caco-2
Anita Hafner1, Jasmina Lovrić, Dario Voinovich
1Department of Pharmaceutics, Faculty of Pharmacy & Biochemistry, University of Zagreb, A. Kovacica 1, 10000 Zagreb, Croatia. ahafner@pharma.hr
International Journal of Pharmaceutics
|July 15, 2009
Summary
Lecithin/chitosan nanoparticles effectively deliver melatonin transmucosally. Optimized nanoparticles significantly enhanced melatonin permeability across the epithelial barrier with no observed toxicity.
Area of Science:
- Drug Delivery and Nanotechnology
- Biomaterials Science
- Pharmacology
Background:
- Transmucosal drug delivery offers an alternative route for systemic administration.
- Melatonin, a hormone with therapeutic potential, faces challenges in oral bioavailability and targeted delivery.
- Developing effective nanocarriers is crucial for improving transmucosal drug absorption.
Purpose of the Study:
- To investigate lecithin/chitosan nanoparticles (NPs) for transmucosal melatonin delivery.
- To characterize NPs based on lecithin type and chitosan content.
- To evaluate melatonin loading, release kinetics, permeability, and safety.
Main Methods:
- Nanoparticle characterization (size, zeta potential, drug loading).
- In vitro release studies.
- Caco-2 cell model for permeability assessment.
- Cell viability assays (MTT, LDH leakage).
Main Results:
- NPs exhibited sizes between 121.6-347.5 nm and zeta potentials of 7.5-32.7 mV.
- Melatonin loading reached up to 7.1% with prolonged release profiles.
- Melatonin permeability was significantly enhanced by NPs (L/C ratio 20:1, Lipoid S45), with no observed cytotoxicity.
Conclusions:
- Lecithin/chitosan NPs are a promising mucoadhesive nanosystem for transmucosal melatonin delivery.
- Optimized NP formulation (Lipoid S45, L/C 20:1) significantly improved melatonin permeability.
- The developed NPs demonstrated safety for Caco-2 cells, indicating potential for transmucosal applications.
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