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[可吸入纳米制剂的进展]

[Advances in inhalable nano-formulations].

作者信息

Luo Yinjia, Yue Xiao, Zhao Ziyu, Zhang Xuejuan

机构信息

College of Pharmacy, Jinan University, Guangzhou 510632, China.

State Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, Jinan University, Guangzhou 510632, China.

出版信息

Zhejiang Da Xue Xue Bao Yi Xue Ban. 2025 Jul 3;54(4):511-521. doi: 10.3724/zdxbyxb-2024-0650.


DOI:10.3724/zdxbyxb-2024-0650
PMID:40665629
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12382326/
Abstract

Nano-drug delivery systems offer significant benefits, including high specific surface area, structural and functional diversity, and surface modifiability. When formulated as inhalable nano-formulation, these can not only enable precise pulmonary drug delivery but also improve pulmonary bioavailability and enhance thera-peutic efficacy. Currently, there are four types of inhalable nano-formulations for the treatment of respiratory diseases. Inhalable liquid preparations exhibit facile manufactur-ability and broad applicability yet demonstrate compromised stability during aerosolization. Through structure optimization, surface modification, dispersion medium optimization and device improvement, the atomization stability of nano-drug has been enhanced. Pressurized metered-dose inhalers loaded with nano-drugs face technical challenges: conventional propellants may dissolve nano-carriers, whereas co-solvents like ethanol compromise delivery efficiency. Thus, it is necessary to develop novel propellants that provide thermodynamic stability and optimal delivery performance. Nano-drug formulations in dry powder inhalers exhibit relatively favorable physical stability, however, pulmonary delivery efficiency and nanoparticles integrity during processing remain problematic. Pulmonary delivery efficiency can be improved by employing strategies such as blending excipients to promote the re-dispersibility of nanoparticle agglomerates, optimizing the design of microcarrier, and innovating preparation processes. In contrast, soft mist inhalers are an ideal option for pulmonary delivery of nano-drugs owing to their gentle and efficient atomization properties to maintain nano-drug integrity. This review summarizes the inhalable nano-formulations and focuses on challenges and proposed strategies encoun-tered in integrating nano-drug delivery systems and inhalation drug delivery systems. It aims to provide references for the future development of inhalable nano-formulations.

摘要

纳米药物递送系统具有显著优势,包括高比表面积、结构和功能多样性以及表面可修饰性。当制成可吸入纳米制剂时,这些不仅可以实现精确的肺部药物递送,还能提高肺部生物利用度并增强治疗效果。目前,有四种用于治疗呼吸系统疾病的可吸入纳米制剂。可吸入液体制剂具有易于制造和广泛适用性,但在雾化过程中稳定性较差。通过结构优化、表面修饰、分散介质优化和装置改进,纳米药物的雾化稳定性得到了提高。装载纳米药物的压力定量吸入器面临技术挑战:传统推进剂可能会溶解纳米载体,而乙醇等助溶剂会降低递送效率。因此,有必要开发具有热力学稳定性和最佳递送性能的新型推进剂。干粉吸入器中的纳米药物制剂表现出相对良好的物理稳定性,然而,在加工过程中的肺部递送效率和纳米颗粒完整性仍然存在问题。可以通过采用混合赋形剂以促进纳米颗粒团聚体的再分散性、优化微载体设计和创新制备工艺等策略来提高肺部递送效率。相比之下,软雾吸入器因其温和高效的雾化特性以保持纳米药物完整性,是纳米药物肺部递送的理想选择。本综述总结了可吸入纳米制剂,并重点关注了纳米药物递送系统与吸入药物递送系统整合中遇到的挑战和提出的策略。旨在为可吸入纳米制剂的未来发展提供参考。

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本文引用的文献

[1]
Precision nanomedicine for pneumonocyte-targeting: Emerging strategies and clinical prospects in refractory pulmonary disease therapy.

Biomaterials. 2025-12

[2]
Zwitterionic Polymer-Functionalized Lipid Nanoparticles for the Nebulized Delivery of mRNA.

J Am Chem Soc. 2024-11-27

[3]
Charge-assisted stabilization of lipid nanoparticles enables inhaled mRNA delivery for mucosal vaccination.

Nat Commun. 2024-11-2

[4]
Double Braking Effects of Nanomedicine on Mitochondrial Permeability Transition Pore for Treating Idiopathic Pulmonary Fibrosis.

Adv Sci (Weinh). 2024-12

[5]
Inhalable polysorbates stabilized nintedanib nanocrystals to facilitate pulmonary nebulization and alveolar macrophage evasion.

Biomater Adv. 2025-1

[6]
Continuously producible aztreonam-loaded inhalable lipid nanoparticles for cystic fibrosis-associated Pseudomonas aeruginosa infections - Development and in-vitro characterization.

Biomater Adv. 2025-1

[7]
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Int J Pharm. 2024-11-15

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Inhalable mRNA Nanoparticle with Enhanced Nebulization Stability and Pulmonary Microenvironment Infiltration.

ACS Nano. 2024-9-3

[9]
Optimized inhaled LNP formulation for enhanced treatment of idiopathic pulmonary fibrosis via mRNA-mediated antibody therapy.

Nat Commun. 2024-8-10

[10]
Advances in nanomaterial-targeted treatment of acute lung injury after burns.

J Nanobiotechnology. 2024-6-18

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