A novel inhalable tanshinone IIA lipid nanocrystal formulation for the enhanced treatment of idiopathic pulmonary fibrosis.
7 affiliations
- 1State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang, 561113, China.
- 2Guizhou Provincial Key Laboratory of Innovation and Manufacturing for Pharmaceuticals, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guiyang, 561113, China.
- 3State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang, 561113, China. [email protected].
- 4Guizhou Provincial Key Laboratory of Innovation and Manufacturing for Pharmaceuticals, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guiyang, 561113, China. [email protected].
- 5State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang, 561113, China. [email protected].
- 6State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang, 561113, China. [email protected].
- 7Guizhou Provincial Key Laboratory of Innovation and Manufacturing for Pharmaceuticals, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guiyang, 561113, China. [email protected].
Abstract
Idiopathic pulmonary fibrosis (IPF) is a progressive, fatal interstitial lung disease marked by relentless deterioration of pulmonary function. Clinically, oral pharmacotherapy for IPF is hampered by two major limitations: inefficient drug delivery to the lung parenchyma and systemic exposure leading to unavoidable off-target side effects. In this study, we developed an inhalable tanshinone IIA (TA) formulation based on lipid nanocrystals to address these challenges. Leveraging the high drug loading capacity and structural stability of lipid nanocrystals, this platform overcomes the intrinsic hydrophobicity of TA, thereby markedly improving its aqueous dispersibility, aerosolization performance, and regional deposition in the deep lung. In vitro, TA lipid nanocrystals significantly enhanced cellular uptake in both pulmonary epithelial cells and lung fibroblasts. In vivo, they achieved substantially high and sustained pulmonary drug exposure. In a bleomycin-induced mouse model of IPF, inhaled TA lipid nanocrystals attenuated histopathological fibrosis, preserved lung function, and suppressed chronic inflammation via modulating the PI3K-Akt signaling pathway and the coagulation-fibrinolysis system. Collectively, this study establishes TA as a promising inhaled therapeutic agent for IPF and introduces lipid nanocrystals as a versatile, scalable, and clinically translatable platform for targeted pulmonary delivery in fibrotic and other chronic respiratory diseases.
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BibTeX
@article{wang2026novel,
title = {{A novel inhalable tanshinone IIA lipid nanocrystal formulation for the enhanced treatment of idiopathic pulmonary fibrosis.}},
author = {Qin Wang and Yun Zhao and Yuanhu Mao and Xiaobo Zhang and Lei Huang and Lei Tang and Yi Chen and Zipeng Gong and Jianqing Peng},
journal = {Journal of nanobiotechnology},
year = {2026},
month = jul,
doi = {10.1186/s12951-026-04786-4},
url = {https://europepmc.org/article/MED/42902239},
note = {CC BY-NC-ND},
}
RIS
TY - JOUR
TI - A novel inhalable tanshinone IIA lipid nanocrystal formulation for the enhanced treatment of idiopathic pulmonary fibrosis.
AU - Qin Wang
AU - Yun Zhao
AU - Yuanhu Mao
AU - Xiaobo Zhang
AU - Lei Huang
AU - Lei Tang
AU - Yi Chen
AU - Zipeng Gong
AU - Jianqing Peng
PY - 2026
DA - 2026/07/01
JO - Journal of nanobiotechnology
DO - 10.1186/s12951-026-04786-4
UR - https://europepmc.org/article/MED/42902239
AB - Idiopathic pulmonary fibrosis (IPF) is a progressive, fatal interstitial lung disease marked by relentless deterioration of pulmonary function. Clinically, oral pharmacotherapy for IPF is hampered by two major limitations: inefficient drug delivery to the lung parenchyma and systemic exposure leading to unavoidable off-target side effects. In this study, we developed an inhalable tanshinone IIA (TA) formulation based on lipid nanocrystals to address these challenges. Leveraging the high drug loading capacity and structural stability of lipid nanocrystals, this platform overcomes the intrinsic hydrophobicity of TA, thereby markedly improving its aqueous dispersibility, aerosolization performance, and regional deposition in the deep lung. In vitro, TA lipid nanocrystals significantly enhanced cellular uptake in both pulmonary epithelial cells and lung fibroblasts. In vivo, they achieved substantially high and sustained pulmonary drug exposure. In a bleomycin-induced mouse model of IPF, inhaled TA lipid nanocrystals attenuated histopathological fibrosis, preserved lung function, and suppressed chronic inflammation via modulating the PI3K-Akt signaling pathway and the coagulation-fibrinolysis system. Collectively, this study establishes TA as a promising inhaled therapeutic agent for IPF and introduces lipid nanocrystals as a versatile, scalable, and clinically translatable platform for targeted pulmonary delivery in fibrotic and other chronic respiratory diseases.
SN - 1477-3155
ER -