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Inhalation Lenalidomide-Loaded Liposome for Bleomycin-Induced Pulmonary Fibrosis Improvement

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Abstract

Idiopathic pulmonary fibrosis (IPF) is a progressive, fibrotic interstitial lung disease with unclear etiology and increasing prevalence. Pulmonary administration can make the drug directly reach the lung lesion location and reduce systemic toxic and side effects. The effectiveness of lenalidomide (Len) liposomal lung delivery in idiopathic pulmonary fibrosis was investigated. Len liposomes (Len-Lip) were prepared from soybean lecithin, cholesterol (Chol), and medicine in different weight ratios by thin film hydration method. The Len-Lip were spherical in shape with an average size of 226.7 ± 1.389 nm. The liposomes with a higher negative zeta potential of around − 34 mV, which was conducive to improving stability by repelling each other. The drug loading and encapsulation rate were 2.42 ± 0.07% and 85.47 ± 2.42%. Len-Lip had little toxicity at the cellular level and were well taken up by cells. At bleomycin-induced pulmonary fibrosis model mice, inhalation Len-Lip could improve lung function and decrease lung hydroxyproline contents, and alleviate pulmonary fibrosis state. Inhalation Len-Lip provided a reference for the treatment of idiopathic pulmonary fibrosis.

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The data of “Inhalation Lenalidomide-Loaded Liposome for Bleomycin-Induced Pulmonary Fibrosis Improvement” can be used by AAPS PharmSciTech.

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Funding

This work was supported by the National Natural Science Foundation of China (81803458), the Fundamental Research Funds for the Central Universities, Nankai University (63231203), the Fundamental Research Funds for the Central Universities, Nankai University (63231200), and the Natural Science Foundation of Tianjin (22JCQNJC01610).

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  1. Zhilin Luo and Liyuan Ji contributed equally to this study.

Authors and Affiliations

  1. College of Pharmacy, Nankai University, No. 38 Tongyan Road, Haihe Education Park, Jinnan District, Tianjin, 300350, China

    Zhilin Luo, Liyuan Ji, Hongting Liu, Yao Sun, Conglu Zhao, Xiang Xu, Xiaoting Gu, Xiaoyu Ai & Cheng Yang

  2. Tianjin Key Laboratory of Molecular Drug Research, Tianjin International Joint Academy of Biomedicine, Tianjin, China

    Zhilin Luo, Hongting Liu, Yao Sun, Conglu Zhao & Xiang Xu

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  1. Zhilin Luo
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  3. Hongting Liu
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  7. Xiaoting Gu
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Contributions

ZL and LJ: conducting the experiments and data acquisition and analysis and writing the original manuscript. HL, YS, CZ, and XX: assisting in the experiments, data acquisition, and literature search. XA, XG, and CY: review, editing, guidance, and supervision.

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Correspondence to Xiaoting Gu, Xiaoyu Ai or Cheng Yang.

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Luo, Z., Ji, L., Liu, H. et al. Inhalation Lenalidomide-Loaded Liposome for Bleomycin-Induced Pulmonary Fibrosis Improvement. AAPS PharmSciTech 24, 235 (2023). https://doi.org/10.1208/s12249-023-02690-w

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