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通过喷雾干燥将纳米晶体封装在基于甘露醇的可吸入微粒中:一种用于姜黄素肺部递送的有前景的策略。

Encapsulation of Nanocrystals in Mannitol-Based Inhalable Microparticles via Spray-Drying: A Promising Strategy for Lung Delivery of Curcumin.

作者信息

Casula Luca, Craparo Emanuela Fabiola, Lai Eleonora, Scialabba Cinzia, Valenti Donatella, Schlich Michele, Sinico Chiara, Cavallaro Gennara, Lai Francesco

机构信息

Department of Life and Environmental Sciences, University of Cagliari, S.P. Monserrato-Sestu km 0.700, Monserrato, 09042 Cagliari, Italy.

Laboratory of Biocompatible Polymers, Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, Italy.

出版信息

Pharmaceuticals (Basel). 2024 Dec 18;17(12):1708. doi: 10.3390/ph17121708.

Abstract

BACKGROUND/OBJECTIVES: Curcumin is well known for its great anti-inflammatory and antioxidant efficacy, representing a potential strategy for the treatment of respiratory disorders. However, several drawbacks, such as chemical instability, poor water solubility and rapid metabolism, result in low bioavailability, limiting its clinical applications. In this study, curcumin nanocrystals were incorporated into mannitol-based microparticles to obtain an inhalable dry powder.

METHODS

A curcumin nanosuspension was produced by wet-ball media milling and thoroughly characterized. Spray drying was then used to produce mannitol microparticles incorporating curcumin nanocrystals. In vitro release/dissolution tests were carried out in simulated lung fluids, and the aerosolization properties were evaluated using a Next-Generation Impactor (NGI, Apparatus E Ph. Eu.).

RESULTS

The incorporation of curcumin nanocrystals into mannitol-based microparticles influenced their morphological properties, such as geometric diameters, and flowability. Despite these changes, nebulization studies confirmed optimal MMAD values (<5 µm), while multi-step dissolution/release studies evidenced the influence of mannitol.

CONCLUSIONS

The developed curcumin nanocrystals-loaded mannitol microparticles show promise as an inhalable treatment for respiratory diseases, combining effective aerodynamic properties with controlled drug release.

摘要

背景/目的:姜黄素以其强大的抗炎和抗氧化功效而闻名,是治疗呼吸系统疾病的一种潜在策略。然而,姜黄素存在一些缺点,如化学稳定性差、水溶性低和代谢迅速,导致其生物利用度低,限制了其临床应用。在本研究中,将姜黄素纳米晶体掺入基于甘露醇的微粒中,以获得可吸入的干粉。

方法

通过湿球介质研磨制备姜黄素纳米混悬液,并对其进行全面表征。然后采用喷雾干燥法制备掺入姜黄素纳米晶体的甘露醇微粒。在模拟肺液中进行体外释放/溶出试验,并使用下一代撞击器(NGI,欧洲药典装置E)评估雾化性能。

结果

将姜黄素纳米晶体掺入基于甘露醇的微粒中会影响其形态学性质,如几何直径和流动性。尽管有这些变化,但雾化研究证实了最佳的质量中值空气动力学直径值(<5μm),而多步溶解/释放研究证明了甘露醇的影响。

结论

所制备的载姜黄素纳米晶体的甘露醇微粒有望作为呼吸系统疾病的可吸入治疗药物,兼具有效的空气动力学性质和可控的药物释放。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/108e/11676507/ab948cf6588e/pharmaceuticals-17-01708-g001.jpg

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