Exploiting marine phospholipid nanoliposomes for enhanced apremilast delivery and therapeutic efficacy in inflammatory bowel disease

IF 5.4 2区化学 Q2 CHEMISTRY, PHYSICAL Colloids and Surfaces A: Physicochemical and Engineering Aspects Pub Date : 2025-08-20 Epub Date: 2025-04-16 DOI:10.1016/j.colsurfa.2025.136967

Samah Shabana , Hamed I. Hamouda , Heng Yin , Samia Hamouda , Busati Ahmed , Mohamed H. El-Sayed , Zhe Chi , Chenguang Liu

{"title":"Exploiting marine phospholipid nanoliposomes for enhanced apremilast delivery and therapeutic efficacy in inflammatory bowel disease","authors":"Samah Shabana , Hamed I. Hamouda , Heng Yin , Samia Hamouda , Busati Ahmed , Mohamed H. El-Sayed , Zhe Chi , Chenguang Liu","doi":"10.1016/j.colsurfa.2025.136967","DOIUrl":null,"url":null,"abstract":"<div><div>Marine phospholipid (MPL) nanoliposomes represent a new frontier in drug delivery systems, offering unique bio-functional and physicochemical properties. This study developed orally administered MPL nanoliposomes to enhance apremilast delivery and bioavailability in inflamed bowel disease (IBD). Drug release studies showed effective gastric protection (21.2 ± 0.4 % release at pH 1.2 after 2 h) and substantial release (96.4 ± 0.3 %) at pH 6.8 over 12 h. The optimized formulation (4 % drug w/w) showed remarkable stability over 6 weeks of storage at 4 °C. Apr/MPL nanoliposomes up to 300 µg/mL showed great cytocompatibility to RAW 264.7 macrophages and Caco2 intestinal cells. Furthermore, the formulation exhibited superior anti-inflammatory effects, significantly reducing nitric oxide (NO) production and downregulating pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. <em>In vivo</em>, Apr/MPL nanoliposomes improved recovery in a dextran sulfate sodium (DSS)-induced ulcerative colitis model, outperforming free apremilast. These findings underscore MPL nanoliposomes as a promising pharmacological tool for managing inflammation and a versatile drug delivery system for IBD.</div></div>","PeriodicalId":278,"journal":{"name":"Colloids and Surfaces A: Physicochemical and Engineering Aspects","volume":"719 ","pages":"Article 136967"},"PeriodicalIF":5.4000,"publicationDate":"2025-08-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Colloids and Surfaces A: Physicochemical and Engineering Aspects","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0927775725008702","RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/4/16 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"CHEMISTRY, PHYSICAL","Score":null,"Total":0}

引用次数: 0

Abstract

Marine phospholipid (MPL) nanoliposomes represent a new frontier in drug delivery systems, offering unique bio-functional and physicochemical properties. This study developed orally administered MPL nanoliposomes to enhance apremilast delivery and bioavailability in inflamed bowel disease (IBD). Drug release studies showed effective gastric protection (21.2 ± 0.4 % release at pH 1.2 after 2 h) and substantial release (96.4 ± 0.3 %) at pH 6.8 over 12 h. The optimized formulation (4 % drug w/w) showed remarkable stability over 6 weeks of storage at 4 °C. Apr/MPL nanoliposomes up to 300 µg/mL showed great cytocompatibility to RAW 264.7 macrophages and Caco2 intestinal cells. Furthermore, the formulation exhibited superior anti-inflammatory effects, significantly reducing nitric oxide (NO) production and downregulating pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. In vivo, Apr/MPL nanoliposomes improved recovery in a dextran sulfate sodium (DSS)-induced ulcerative colitis model, outperforming free apremilast. These findings underscore MPL nanoliposomes as a promising pharmacological tool for managing inflammation and a versatile drug delivery system for IBD.

查看原文

微信好友朋友圈 QQ好友复制链接

本刊更多论文

利用海洋磷脂纳米脂质体增强阿普米司特在炎症性肠病中的传递和治疗效果

海洋磷脂（MPL）纳米脂质体具有独特的生物功能和物理化学性质，是药物传递系统研究的新领域。本研究开发了口服MPL纳米脂质体，以增强炎症性肠病（IBD）的阿普米司特递送和生物利用度。药物释放研究表明，在pH为1.2时，2 h后释放量为21.2 ± 0.4 %；在pH为6.8时，12 h后释放量为96.4 ± 0.3 %。优化后的配方（4 %药物w/w）在4 °C下保存6周，稳定性显著。Apr/MPL纳米脂质体浓度高达300 µg/mL，对RAW 264.7巨噬细胞和Caco2肠细胞具有良好的细胞相容性。此外，该制剂具有卓越的抗炎作用，可显著降低脂多糖（LPS）刺激的RAW 264.7巨噬细胞中一氧化氮（NO）的产生，并下调促炎细胞因子（TNF-α, IL-1β, IL-6）。在体内，Apr/MPL纳米脂质体改善了葡聚糖硫酸钠（DSS）诱导的溃疡性结肠炎模型的恢复，优于游离阿普米司特。这些发现强调了MPL纳米脂质体作为一种有前途的控制炎症的药理学工具和IBD的多功能药物输送系统。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文去求助

来源期刊

Colloids and Surfaces A: Physicochemical and Engineering Aspects 化学-物理化学

CiteScore

8.70

自引率

9.60%

发文量

2421

审稿时长

56 days

期刊介绍： Colloids and Surfaces A: Physicochemical and Engineering Aspects is an international journal devoted to the science underlying applications of colloids and interfacial phenomena. The journal aims at publishing high quality research papers featuring new materials or new insights into the role of colloid and interface science in (for example) food, energy, minerals processing, pharmaceuticals or the environment.