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May 9, 2026Sci1 citationsOpen Access

Natural Deep Eutectic Solvent-Based Eutectogels for Enhanced Colon-Targeted Delivery of Mesalazine

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RSRoberta Del SoleRCRoberta CassanoCSCarlo Siciliano

Key Points

  • To enhance the oral bioavailability of mesalazine through the development of a novel eutectogel delivery system.
  • Developed a eutectogel using choline chloride and lactic acid with hydroxyethyl cellulose and Carbomer 140.
  • Coated the gel matrix with Eudragit® S100 for controlled pH release.
  • Conducted physicochemical characterization and in vitro release studies in simulated gastrointestinal conditions.
  • Mesalazine solubility increased to 35 mg/mL, approximately 40 times higher than in water.
  • At gastric pH (1.2), minimal drug release was observed, while sustained release exceeded 80% at colonic pH (7.4) over 48 hours.
  • The system demonstrates biocompatibility and potential for effective colon-targeted drug delivery.

Abstract

Poor solubility and low permeability remain major obstacles to the oral bioavailability of mesalazine (5-aminosalicylic acid, 5-ASA), a BCS Class IV anti-inflammatory drug used in the treatment of inflammatory bowel diseases. In this study, we report a novel eutectogel (EG) platform based on a natural deep eutectic solvent (NADES) composed of choline chloride and lactic acid (ChCl:LA, 1:10 molar ratio). The NADES significantly enhanced mesalazine solubility, reaching 35 mg/mL, nearly 40-fold higher than in water. The drug-loaded NADES was structured using hydroxyethyl cellulose and Carbomer 140 to obtain a gel matrix, which was subsequently coated with Eudragit® S100 to provide pH-dependent release and gastro-resistance. Physicochemical characterization was carried out via FT-IR and NMR spectroscopy, polarized optical microscopy (POM), and swelling studies in simulated fluids. In vitro release studies under simulated gastrointestinal conditions revealed minimal drug release at gastric pH (1.2) and a sustained release (>80%) at colonic pH (7.4) over 48 h. These results support the potential of ChCl:LA-based eutectogels as a biocompatible, green, and effective delivery system for the site-specific release of poorly soluble drugs in the colon.

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Cite This Study

Sole et al. (2026) studied this question.

synapsesocial.com/papers/69fecfafb9154b0b82876ad5https://doi.org/10.3390/sci8050106
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