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负载苯并[k,l]呫吨木脂素的固体脂质纳米粒的表征及其与生物膜模型的相互作用

Characterization and Interaction with Biomembrane Model of Benzo[k,l]xanthene Lignan Loaded Solid Lipid Nanoparticles.

作者信息

Torrisi Cristina, Cardullo Nunzio, Muccilli Vera, Tringali Corrado, Castelli Francesco, Sarpietro Maria Grazia

机构信息

Department of Drug and Health Sciences, University of Catania, Viale Andrea Doria 6, 95125 Catania, Italy.

Department of Chemical Sciences, University of Catania, Viale Andrea Doria 6, 95125 Catania, Italy.

出版信息

Membranes (Basel). 2022 Jun 13;12(6):615. doi: 10.3390/membranes12060615.

Abstract

Benzo[k,l]xanthene lignans are a group of rare natural products belonging to the class of polyphenols with promising biological activities and are studied as potential chemotherapeutic agents. The lipophilic character of a xanthene core makes these molecules difficult to be used in an aqueous medium, limiting their employment in studies for pharmaceutical applications. To overcome this problem, a drug-delivery system which is able to improve the stability and bioavailability of the compound can be used. In this study, a bioactive benzoxanthene lignan (BXL) has been included in SLN. Unloaded and BXL-loaded SLN have been prepared using the Phase Inversion Temperature method and characterized in terms of size, zeta potential, entrapment efficiency and stability. Differential scanning calorimetry was used to evaluate the thermotropic behavior and ability of SLN to act as carriers for BXL. A biomembrane model, represented by multilamellar vesicles, was used to simulate the interaction of the SLN with the cellular membrane. Unloaded and loaded SLN were incubated with the MLV, and their interactions were evaluated through variations in their calorimetric curves. The results obtained suggest that SLN could be used as a delivery system for BXL.

摘要

苯并[k,l]呫吨木脂素是一类稀有的天然产物,属于具有潜在生物活性的多酚类,作为潜在的化学治疗剂受到研究。呫吨核心的亲脂性使得这些分子难以在水性介质中使用,限制了它们在药物应用研究中的应用。为克服这一问题,可使用能够提高该化合物稳定性和生物利用度的药物递送系统。在本研究中,一种生物活性苯并呫吨木脂素(BXL)已被载入固体脂质纳米粒(SLN)。采用相转变温度法制备了未载药和载有BXL的SLN,并对其粒径、ζ电位、包封率和稳定性进行了表征。差示扫描量热法用于评估SLN的热致行为以及作为BXL载体的能力。以多层囊泡为代表的生物膜模型用于模拟SLN与细胞膜的相互作用。将未载药和载药的SLN与多层囊泡(MLV)一起孵育,并通过量热曲线的变化评估它们的相互作用。所得结果表明,SLN可用作BXL的递送系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e80/9227282/bd135f1c7a58/membranes-12-00615-sch001.jpg

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