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Updated: Aug 6, 2026
08:44
Preparation, Administration, and Assessment of In Vivo Tissue-Specific Cellular Uptake of Fluorescent Dye-Labeled Liposomes
Published on: July 30, 2020
Roxadustat-loaded pH-sensitive Anionic Liposomes Ameliorating Experimental Colitis in Mice: Formulation, Cellular
Guiping Kong1, Yucan Zheng1, Yan Lu1
1Department of Gastroenterology, Children's Hospital of Nanjing Medical University, Nanjing 210008, Jiangsu, China.
Current Drug Delivery
|July 20, 2026
Summary
This study developed pH-responsive nanocarriers (ROX-MAE@LP) to improve roxadustat's oral delivery for colitis treatment. The nanocarriers enhanced bioavailability and therapeutic efficacy in inflammatory bowel disease models.
Area of Science:
- Nanomedicine
- Pharmaceutical Sciences
- Gastroenterology
Background:
- Roxadustat, a hypoxia-inducible factor prolyl hydroxylase inhibitor, shows promise for colitis but suffers from poor water solubility and rapid gastrointestinal absorption.
- These limitations hinder its clinical application for inflammatory bowel disease (IBD).
Purpose of the Study:
- To develop a pH-responsive, intestinal-targeted nanocarrier system for roxadustat.
- To enhance the oral bioavailability and anti-colitis efficacy of roxadustat.
Main Methods:
- Roxadustat-loaded liposomes (ROX-LP) were formulated and coated with Kollicoat MAE 100 P to create pH-responsive nanoparticles (ROX-MAE@LP).
- The formulation underwent evaluation for physicochemical properties, in vitro drug release, cellular uptake, pharmacokinetics, and in vivo therapeutic efficacy in a colitis model.
Main Results:
- ROX-MAE@LP exhibited excellent encapsulation, spherical morphology, and pH-dependent release, with increased release at intestinal pH.
- Significant enhancement in oral bioavailability and prolonged mean residence time were observed for ROX-MAE@LP compared to roxadustat suspension.
- ROX-MAE@LP demonstrated superior anti-inflammatory effects, reduced pro-inflammatory cytokines, and promoted mucosal repair in a murine colitis model.
Conclusions:
- The pH-responsive, intestinal-targeted nanocarrier system (ROX-MAE@LP) effectively overcomes roxadustat's limitations, improving its local intestinal concentration and therapeutic outcomes.
- This formulation holds significant potential for oral therapy in inflammatory bowel disease and offers new avenues for developing advanced nanocarrier systems.
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