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已发表论文
双靶向口服药物负载纳米结构脂质载体增强溃疡性结肠炎疗效
Authors Liu M, Cui J, Li H, Yang J, Liu G
Received 21 June 2025
Accepted for publication 10 October 2025
Published 18 October 2025 Volume 2025:20 Pages 12681—12697
DOI https://doi.org/10.2147/IJN.S548696
Checked for plagiarism Yes
Review by Single anonymous peer review
Peer reviewer comments 3
Editor who approved publication: Prof. Dr. RDK Misra
Meijia Liu, Junyi Cui, Hanqing Li, Jie Yang, Guoyun Liu
State Key Laboratory of Macromolecular Drugs and Large-Scale Preparation, School of Pharmaceutical Sciences and Food Engineering, Liaocheng University, Liaocheng, Shandong, 252059, People’s Republic of China
Correspondence: Guoyun Liu, Email liuguoyun@lcu.edu.cn Jie Yang, Email yangjie3@lcu.edu.cn
Purpose: Ulcerative colitis (UC) is a non-specific inflammatory intestinal disease with long course and easy recurrence, which is one of the refractory diseases. In the previous work, para-quinone methide compound p-QM- 1i was found to be a potential anti-UC drug in UC mice; however, its water solubility was poor, and the oral dosage was high. In this study, in response to these shortcomings, an oral, actively targeted, and drug-loaded nanostructured lipid carrier (NLC) was constructed, and the dual-stage targeted design was performed on it.
Methods: Firstly, the p-QM- 1i-loaded NLC surface was modified with infliximab (IFX) (p-QM- 1i-IFX-NLC), which can target highly expressed TNF-α in inflammatory cells or tissues; secondly, p-QM- 1i-IFX-NLC was coated with Eudragit S100 (S100- 1i-IFX-NLC), which can achieve specific release in the colon and protect NLC from interference from the gastrointestinal environment.
Results: The experimental results suggested that the dual-stage targeted design of S100- 1i-IFX-NLC can effectively increase the solubility of p-QM- 1i, allowing S100- 1i-IFX-NLC to target the colon and p-QM- 1i-IFX-NLC to target the inflammatory tissue, increasing the aggregation of p-QM- 1i in the colon, enhancing the efficacy of p-QM- 1i, reducing the usage of p-QM- 1i, and increasing safety.
Conclusion: The construction of Eudragit S100-coated p-QM- 1i-loaded IFX-modified NLC (S100- 1i-IFX-NLC) was effective and can improve the therapeutic effect of free drugs on UC.
Keywords: ulcerative colitis, nanostructured lipid carriers, target delivery, TNF-α, colon specific release
State Key Laboratory of Macromolecular Drugs and Large-Scale Preparation, School of Pharmaceutical Sciences and Food Engineering, Liaocheng University, Liaocheng, Shandong, 252059, People’s Republic of China
Correspondence: Guoyun Liu, Email liuguoyun@lcu.edu.cn Jie Yang, Email yangjie3@lcu.edu.cn
Purpose: Ulcerative colitis (UC) is a non-specific inflammatory intestinal disease with long course and easy recurrence, which is one of the refractory diseases. In the previous work, para-quinone methide compound p-QM- 1i was found to be a potential anti-UC drug in UC mice; however, its water solubility was poor, and the oral dosage was high. In this study, in response to these shortcomings, an oral, actively targeted, and drug-loaded nanostructured lipid carrier (NLC) was constructed, and the dual-stage targeted design was performed on it.
Methods: Firstly, the p-QM- 1i-loaded NLC surface was modified with infliximab (IFX) (p-QM- 1i-IFX-NLC), which can target highly expressed TNF-α in inflammatory cells or tissues; secondly, p-QM- 1i-IFX-NLC was coated with Eudragit S100 (S100- 1i-IFX-NLC), which can achieve specific release in the colon and protect NLC from interference from the gastrointestinal environment.
Results: The experimental results suggested that the dual-stage targeted design of S100- 1i-IFX-NLC can effectively increase the solubility of p-QM- 1i, allowing S100- 1i-IFX-NLC to target the colon and p-QM- 1i-IFX-NLC to target the inflammatory tissue, increasing the aggregation of p-QM- 1i in the colon, enhancing the efficacy of p-QM- 1i, reducing the usage of p-QM- 1i, and increasing safety.
Conclusion: The construction of Eudragit S100-coated p-QM- 1i-loaded IFX-modified NLC (S100- 1i-IFX-NLC) was effective and can improve the therapeutic effect of free drugs on UC.
Keywords: ulcerative colitis, nanostructured lipid carriers, target delivery, TNF-α, colon specific release