Inulin Amphiphilic Copolymer-Based Drug Delivery: Unraveling the Structural Features of Graft Constructs

• Main Authors: Carla Sardo (Author), Giulia Auriemma (Author), Carmela Mazzacano (Author), Claudia Conte (Author), Virgilio Piccolo (Author), Tania Ciaglia (Author), Marta Denel-Bobrowska (Author), Agnieszka B. Olejniczak (Author), Donatella Fiore (Author), Maria Chiara Proto (Author), Patrizia Gazzerro (Author), Rita Patrizia Aquino (Author)
• Format: Book
• Published: MDPI AG, 2024-07-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Summary

In this study, the structural attributes of nanoparticles obtained by a renewable and non-immunogenic "inulinated" analog of the "pegylated" PLA (PEG-PLA) were examined, together with the potential of these novel nanocarriers in delivering poorly water-soluble drugs. Characterization of INU-PLA assemblies, encompassing critical aggregation concentration (CAC), NMR, DLS, LDE, and SEM analyses, was conducted to elucidate the core/shell architecture of the carriers and in vitro cyto- and hemo-compatibility were assayed. The entrapment and in vitro delivery of sorafenib tosylate (<i>ST</i>) were also studied. INU-PLA copolymers exhibit distinctive features: (1) Crew-cut aggregates are formed with coronas of 2-4 nm; (2) a threshold surface density of 1 INU/nm² triggers a configuration change; (3) INU surface density influences PLA core dynamics, with hydrophilic segment stretching affecting PLA distribution towards the interface. INU-PLA₂<i>NPs</i> demonstrated an outstanding loading of <i>ST</i> and excellent biological profile, with effective internalization and <i>ST</i> delivery to HepG2 cells, yielding a comparable IC₅₀.

Item Description

10.3390/pharmaceutics16080971
1999-4923