The knowledge of the interactions between solid lipidnanoparticles (SLN) and cell membranes is important to developeffective carrier systems for drug delivery applications. Loadingidebenone (IDE), an antioxidant drug useful in the treatment ofneurodegenerative diseases, into SLN improves IDE antioxidantactivity in in vitro biological studies, but the mechanism by whichIDE permeation through the blood−brain barrier (BBB) occurs arestill unclear. Therefore, in this research, unloaded and IDE loaded SLNinteraction with biomembrane models, consisting of dimyristoylphosphatidylcholinemultilamellar vesicles (MLV), were studied by differential scanning calorimetry (DSC). In the experimentsperformed, unloaded and IDE loaded SLN where incubated with the biomembrane models and their interactions were evaluatedthrough the variations in their calorimetric curves. The results of our DSC studies indicated that the SLN under investigationwere able to go inside the phospholipid bilayers with a likely localization in the outer bilayers of the MLV from where theymoved toward the inner layers by increasing the contact time between SLN and MLV. Furthermore, IDE loaded SLN were ableto release IDE into the biomembrane model, thus facilitating IDE penetration into the bilayers while free IDE showed only a lowability to interact with this model of biomembranes. Our results suggest that these SLN could be regarded as a promising drugdelivery system to improve IDE bioavailability and antioxidant activity.

Idebenone loaded solid lipid nanoparticles interact with biomembrane models: calorimetric evidence

MONTENEGRO, LUCIA;PUGLISI, Giovanni;CASTELLI, Francesco;SARPIETRO, MARIA GRAZIA
2012-01-01

Abstract

The knowledge of the interactions between solid lipidnanoparticles (SLN) and cell membranes is important to developeffective carrier systems for drug delivery applications. Loadingidebenone (IDE), an antioxidant drug useful in the treatment ofneurodegenerative diseases, into SLN improves IDE antioxidantactivity in in vitro biological studies, but the mechanism by whichIDE permeation through the blood−brain barrier (BBB) occurs arestill unclear. Therefore, in this research, unloaded and IDE loaded SLNinteraction with biomembrane models, consisting of dimyristoylphosphatidylcholinemultilamellar vesicles (MLV), were studied by differential scanning calorimetry (DSC). In the experimentsperformed, unloaded and IDE loaded SLN where incubated with the biomembrane models and their interactions were evaluatedthrough the variations in their calorimetric curves. The results of our DSC studies indicated that the SLN under investigationwere able to go inside the phospholipid bilayers with a likely localization in the outer bilayers of the MLV from where theymoved toward the inner layers by increasing the contact time between SLN and MLV. Furthermore, IDE loaded SLN were ableto release IDE into the biomembrane model, thus facilitating IDE penetration into the bilayers while free IDE showed only a lowability to interact with this model of biomembranes. Our results suggest that these SLN could be regarded as a promising drugdelivery system to improve IDE bioavailability and antioxidant activity.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.11769/40469
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