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巯基化羟丙基-β-环糊精用于肺部药物传递。

Cross-Linked Thiolated Hydroxypropil-β-Cyclodextrin for Pulmonary Drug Delivery.

机构信息

Department of Pharmacy, University of Pisa, Via Bonanno 33, 56126 Pisa, Italy.

Department of Life Sciences, University of Siena, 53100 Siena, Italy.

出版信息

Int J Mol Sci. 2024 Aug 29;25(17):9394. doi: 10.3390/ijms25179394.

DOI:10.3390/ijms25179394
PMID:39273341
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11395519/
Abstract

UNLABELLED

Inhalable formulations with cyclodextrins (CDs) as solubility and absorption enhancers show promise for pulmonary delivery. Thiolated hydroxypropyl-β-cyclodextrin (HP-β-CD-SH) has mucoadhesive properties, enhancing drug absorption. Moreover, it has self-aggregation capability, which could further improve absorption and drug stability, as well as reduce irritation. This study aims to stabilize CD nanoaggregates using bifunctional cross-linkers and evaluate their benefits for lung drug delivery compared to pristine HP-β-CD-SH.

METHODS

The effectiveness of cross-linked HP-β-CD-SH nanoparticles (HP-β-CD-SH-NP) was compared to transient nanoaggregates in enhancing the activity of dexamethasone (DMS) and olive leaf extracts (OLE). DMS, a poorly soluble drug commonly used in lung treatments, and OLE, known for its antioxidant properties, were chosen. Drug-loaded HP-β-CD-SH-NP were prepared and nebulized onto a lung epithelial Air-Liquid Interface (ALI) model, assessing drug permeation and activity.

RESULTS

HP-β-CD-SH with 25% thiolation was synthesized via microwave reaction, forming 150 nm nanoaggregates and stabilized 400 nm HP-β-CD-SH-NP. All carriers showed good complexing ability with DMS and OLE and were biocompatible in the lung ALI model. HP-β-CD-SH promoted DMS absorption, while stabilized HP-β-CD-SH-NP protected against oxidative stress.

CONCLUSION

HP-β-CD-SH is promising for lung delivery, especially as stabilized nanoaggregates, offering versatile administration for labile molecules like natural extracts.

摘要

目的

使用双功能交联剂稳定 CD 纳米聚集体，并评估其与原始 HP-β-CD-SH 相比对肺部药物输送的益处。

方法

比较交联 HP-β-CD-SH 纳米颗粒（HP-β-CD-SH-NP）与瞬态纳米聚集体对地塞米松（DMS）和橄榄叶提取物（OLE）活性的增强作用。选择 DMS 作为肺部治疗中常用的疏水性药物，OLE 作为具有抗氧化特性的药物。制备载药的 HP-β-CD-SH-NP 并雾化到肺上皮细胞气液界面（ALI）模型上，评估药物渗透和活性。

结果

通过微波反应合成了 25%巯基化的 HP-β-CD-SH，形成了 150nm 的纳米聚集体，并稳定了 400nm 的 HP-β-CD-SH-NP。所有载体均表现出与 DMS 和 OLE 的良好结合能力，在肺 ALI 模型中具有生物相容性。HP-β-CD-SH 促进了 DMS 的吸收，而稳定的 HP-β-CD-SH-NP 则能抵抗氧化应激。

结论

HP-β-CD-SH 有望用于肺部输送，特别是作为稳定的纳米聚集体，为不稳定分子（如天然提取物）提供了多种给药途径。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d9c6/11395519/310ecaaa6b45/ijms-25-09394-g007.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d9c6/11395519/b3b58366518d/ijms-25-09394-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d9c6/11395519/310ecaaa6b45/ijms-25-09394-g007.jpg

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4
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