Idebenone Loaded Solid Lipid Nanoparticles Interact with Biomembrane Models: Calorimetric Evidence

固体脂质纳米粒 脂质体 生物膜 艾地苯醌 生物物理学 化学 磷脂 脂质双层 药物输送 差示扫描量热法 小泡 渗透 生物化学 有机化学 生物 物理 热力学
作者
Lucia Montenegro,Sara Ottimo,Giovanni Puglisi,Francesco Castelli,Maria Grazia Sarpietro
出处
期刊:Molecular Pharmaceutics [American Chemical Society]
卷期号:9 (9): 2534-2541 被引量:26
标识
DOI:10.1021/mp300149w
摘要

The knowledge of the interactions between solid lipid nanoparticles (SLN) and cell membranes is important to develop effective carrier systems for drug delivery applications. Loading idebenone (IDE), an antioxidant drug useful in the treatment of neurodegenerative diseases, into SLN improves IDE antioxidant activity in in vitro biological studies, but the mechanism by which IDE permeation through the blood–brain barrier (BBB) occurs are still unclear. Therefore, in this research, unloaded and IDE loaded SLN interaction with biomembrane models, consisting of dimyristoylphosphatidylcholine multilamellar vesicles (MLV), were studied by differential scanning calorimetry (DSC). In the experiments performed, unloaded and IDE loaded SLN where incubated with the biomembrane models and their interactions were evaluated through the variations in their calorimetric curves. The results of our DSC studies indicated that the SLN under investigation were able to go inside the phospholipid bilayers with a likely localization in the outer bilayers of the MLV from where they moved toward the inner layers by increasing the contact time between SLN and MLV. Furthermore, IDE loaded SLN were able to release IDE into the biomembrane model, thus facilitating IDE penetration into the bilayers while free IDE showed only a low ability to interact with this model of biomembranes. Our results suggest that these SLN could be regarded as a promising drug delivery system to improve IDE bioavailability and antioxidant activity.
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