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

被引：1

作者：

Sardo, Carla ^{[1
]}

Auriemma, Giulia ^{[1
]}

Mazzacano, Carmela ^{[1
]}

Conte, Claudia ^{[2
]}

Piccolo, Virgilio ^{[2
]}

Ciaglia, Tania ^{[1
]}

Denel-Bobrowska, Marta ^{[3
]}

Olejniczak, Agnieszka B. ^{[3
]}

Fiore, Donatella ^{[1
]}

Proto, Maria Chiara ^{[1
]}

Gazzerro, Patrizia ^{[1
]}

Aquino, Rita Patrizia ^{[1
]}

机构：

[1] Univ Salerno, Dept Pharm, Via Giovanni Paolo 2 132, I-84084 Fisciano, Italy

[2] Univ Naples Federico II, Dept Pharm, Via Domenico Montesano 49, I-80131 Naples, Italy

[3] Polish Acad Sci, Inst Med Biol, Lodowa 106, PL-93232 Lodz, Poland

来源：

PHARMACEUTICS | 2024年 / 16卷 / 08期

关键词：

PEG alternative; inulin; PLA; sorafenib tosylate; crew-cut nanoparticles; FALT; POLYETHYLENE-GLYCOL; NANOPARTICLES; POLYMER; SURFACE; WELL;

D O I：

10.3390/pharmaceutics16080971

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 (ST) 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 NPs demonstrated an outstanding loading of ST and excellent biological profile, with effective internalization and ST delivery to HepG2 cells, yielding a comparable IC50.

引用

页数：17

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