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Formulation, Characterization, and Cytotoxicity Evaluation of Lactoferrin Functionalized Lipid Nanoparticles for
Maria Inês Teixeira1,2, Carla Martins Lopes3, Hugo Gonçalves4
1Associate Laboratory i4HB-Institute for Health and Bioeconomy, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal.
Pharmaceutics
|January 21, 2022
Summary
Researchers developed lactoferrin-functionalized nanostructured lipid carriers (NLC) to deliver riluzole across the blood-brain barrier for amyotrophic lateral sclerosis (ALS) treatment. These biocompatible NLC show promise for enhanced brain targeting and drug delivery.
Area of Science:
- Neuroscience and Pharmacology
- Biomaterials and Nanotechnology
Background:
- Amyotrophic lateral sclerosis (ALS) is a neurodegenerative disease with limited treatment options.
- The blood-brain barrier (BBB) restricts drug delivery to the brain, hindering effective ALS therapy.
- Riluzole is a common ALS drug with poor brain penetration due to the BBB.
Purpose of the Study:
- To develop a novel drug delivery system for enhanced brain targeting of riluzole.
- To overcome the limitations of the blood-brain barrier for ALS treatment.
- To functionalize nanostructured lipid carriers (NLC) with lactoferrin (Lf) for improved brain endothelial transport.
Main Methods:
- Preparation and characterization of lactoferrin-functionalized nanostructured lipid carriers (Lf-NLC) loaded with riluzole.
- Assessment of physicochemical properties: size, zeta potential, polydispersity index, stability, encapsulation efficiency, morphology (TEM).
- Evaluation of in vitro release, crystallinity (DSC, PXRD), and biocompatibility (MTT assay on NSC-34 and hCMEC/D3 cells).
Main Results:
- Riluzole-loaded Lf-NLC exhibited optimal physicochemical properties with mean diameters of 180-220 nm and narrow size distribution (PDI < 0.3).
- High encapsulation efficiency (94-98%) and stability over 3 months were achieved.
- Lf conjugation was confirmed; Lf-NLC were spherical, biocompatible, and showed potential for BBB transport.
Conclusions:
- Lactoferrin-functionalized nanostructured lipid carriers are a promising, biocompatible system for targeted brain delivery of riluzole.
- This approach offers a potential strategy to improve therapeutic efficacy for amyotrophic lateral sclerosis.
- Lf-NLC facilitate drug transport across the blood-brain barrier via receptor-mediated endocytosis.
