Biomimetic Nanoparticles Carrying EP300 Inhibitor for the Treatment of Idiopathic Pulmonary Fibrosis
Abstract Idiopathic pulmonary fibrosis (IPF) is a progressive, irreversible lung disease with limited treatment options. SGC-CBP30, a CBP/EP300 inhibitor, shows anti-fibrotic activity but suffers from poor bioavailability and tissue specificity. Here, we developed platelet membrane-coated nanoparticles (PNP) for targeted pulmonary delivery of SGC-CBP30 to enhance therapeutic efficacy. PNP was generated by encapsulating SGC-CBP30 in Poly (lactic-co-glycolic acid) (PLGA) nanoparticles coated with platelet membranes. Efficacy, biodistribution, and safety were evaluated in TGF-β1-stimulated PA317 cells and a BLM-induced pulmonary fibrosis model using immunofluorescence, Western blot, histology, PFTs (Pulmonary Function Tests), imaging, and serum biochemistry. PNP suppressed fibrotic markers (COL6A1, α-SMA, FN1, COL1A1) in vitro and showed lung-targeted delivery in vivo, improving lung function and reducing inflammation and fibrosis in BLM mice without detectable toxicity. Lung-targeted CBP/EP300 inhibition by PNP represents a biomimetic, translatable approach for anti-fibrotic therapy with potential extrapolation to other fibrotic diseases.
Authors
- Zhengyi Wei (ORCID: https://orcid.org/0000-0002-6704-939X)
- Lingmin Zhang (ORCID: https://orcid.org/0000-0002-4215-5401)
- Yifan Gong (ORCID: https://orcid.org/0000-0002-1930-443X)
- 杜玲然
- Zizhang Ouyang
- Mei Feng
- Xin-Xiang Chen
- Aiping Qin (ORCID: https://orcid.org/0000-0001-6393-7034)
- Zhida Chen
- Lu Liang
- Jianfen Su
- Yong-hang Fan
Institutions
- Guangzhou University (CN)
- Panyu Hospital of Chinese Medicine (CN)
- Guangzhou Experimental Station (CN)
- Qingzhou City People's Hospital (CN)
- Guangzhou Medical University (CN)
Publication Details
- Journal
- Molecular Pharmaceutics
- Published
- 2026-09-25
- DOI
- https://doi.org/10.1021/acs.molpharmaceut.6c00949
- Primary Topic
- Interstitial Lung Diseases and Idiopathic Pulmonary Fibrosis
- Type
- article
- Field-Weighted Citation Impact
- 0.00