Inhalable stealth liposomes improve peptide delivery for pulmonary fibrosis treatment
文献类型：期刊论文
| 作者 | Lin, Ruibo2,3; Li, Zhengqing2; Sun, Yuelan1,2; Shen, Jianhao1; Cao, Xiang4; Lin, Yongfang2; Fu, Chang2; Zhu, Yugen2; Wang, Chaoqun2; Tan, Zheng2 |
| 刊名 | JOURNAL OF CONTROLLED RELEASE
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| 出版日期 | 2026-03-10 |
| 卷号 | 391页码:15 |
| 关键词 | Pulmonary fibrosis CSP7 Liposome Peptide delivery Inhaled administration |
| ISSN号 | 0168-3659 |
| DOI | 10.1016/j.jconrel.2026.114655 |
| 通讯作者 | Zhang, Jiabin(jiabinzhang@simm.ac.cn) ; Huang, Yongzhuo(yzhuang@simm.ac.cn) ; Shen, Shiyang(shenshiyang@simm.ac.cn) |
| 英文摘要 | Pulmonary fibrosis is a life-threatening lung disease with limited therapeutic options and suboptimal clinical outcomes. Peptide-based agents such as CSP7, a heptapeptide derived from caveolin-1, have shown promising antifibrotic activity with low systemic toxicity. However, effective inhaled administration of CSP7 is impeded by physiological barriers in fibrotic lungs, including alveolar edema fluid and clearance by inflammatory macrophages. Here, we report a high-loading stealth liposomal system designed to enhance pulmonary delivery of CSP7 by inhalation. CSP7 was covalently conjugated to an aliphatic lipid moiety to generate a lipidated prodrug (l-CSP7), enabling markedly improved incorporation into PEGylated stealth liposomes (l-CSP7/Lips) with about 4-fold higher encapsulation efficiency and drug loading. The optimized formulation also exhibited enhanced penetration through edematous alveolar fluid and reduced macrophage clearance. After deposition in the alveoli and uptake by myofibroblasts, intracellular enzymes cleave l-CSP7 to release active CSP7, thereby attenuating profibrotic cellular phenotypes. In bleomycin-induced idiopathic pulmonary fibrosis and silica-induced silicosis animal models, inhaled l-CSP7/Lips achieved superior alveolar delivery and therapeutic outcomes compared with free CSP7 and clinical drug nintedanib, reversing fibrotic remodeling, improving respiratory function, and reducing inflammation and collagen deposition. These results introduce a modular and translatable nanocarrier platform for inhalable peptide therapeutics and support a localized treatment strategy for pulmonary fibrosis and potentially other lung diseases. |
| 资助项目 | National Key Research and Development Program of China[2025YFE0107400] ; National Natural Science Foundation of China[82104090] ; Guangdong Basic and Applied Basic Research Foundation, China[2025A1515010594] ; Social Public Welfare and Basic Research Project of Zhongshan City, China[2024B2016] ; Innovative Scientific Research Team Project of Zhongshan City, China[CXTD2024007] ; National Key Laboratory of Advanced Drug Delivery and Release Systems, China[DSQZ-QN-202302] ; Project of High-level New R & D Institute, Department of Science and Technology of Guangdong Province, China[2019B090904008] ; High-level Innovative Research Institute, Department of Science and Technology of Guangdong Province, China[2021B0909050003] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001678625600002 |
| 出版者 | ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/322743]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Zhang, Jiabin; Huang, Yongzhuo; Shen, Shiyang |
| 作者单位 | 1.Southern Med Univ, Sch Pharmaceut Sci, Guangzhou 510515, Peoples R China 2.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Shanghai Inst Mat Med, Zhongshan 528400, Peoples R China 3.Guangzhou Univ Chinese Med, Sch Chinese Mat Med, Guangzhou 510006, Peoples R China 4.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China 5.Chinese Acad Sci, Shanghai Inst Mat Med, Pharmaceut Preparat Res Ctr, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Lin, Ruibo,Li, Zhengqing,Sun, Yuelan,et al. Inhalable stealth liposomes improve peptide delivery for pulmonary fibrosis treatment[J]. JOURNAL OF CONTROLLED RELEASE,2026,391:15. |
| APA | Lin, Ruibo.,Li, Zhengqing.,Sun, Yuelan.,Shen, Jianhao.,Cao, Xiang.,...&Shen, Shiyang.(2026).Inhalable stealth liposomes improve peptide delivery for pulmonary fibrosis treatment.JOURNAL OF CONTROLLED RELEASE,391,15. |
| MLA | Lin, Ruibo,et al."Inhalable stealth liposomes improve peptide delivery for pulmonary fibrosis treatment".JOURNAL OF CONTROLLED RELEASE 391(2026):15. |
入库方式： OAI收割
来源：上海药物研究所
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