Multicompartmental Hydrogel Microspheres with a Concentric Thin Oil Layer: Protecting and Targeting Therapeutic Agents for Inflammatory Bowel Disease. — VialBase Research

Summary

This study developed multicompartmental hydrogel microspheres with a concentric thin oil layer to improve oral delivery of therapeutic agents for inflammatory bowel disease (IBD). Made from triple-emulsion droplets, the microspheres use intermediate oil layers to separate two prepolymer phases so each compartment can be independently tuned, and a hydrogel core for stability under the stomach’s high osmolarity. The oil layer shields the payload from stomach acid, while a tuned shell enables pH-selective release in the gut. As a proof of concept, the platform preserved the anti-inflammatory activity of both 5-aminosalicylic acid (5-ASA) and KPV under stomach conditions and maintained their effects on colonic epithelial cells.

Key Findings

• Multicompartmental hydrogel microspheres were built from triple-emulsion droplets whose intermediate oil layers distinctly separate two prepolymer phases, allowing each compartment’s composition to be fine-tuned via a tailored polymerization strategy.
• The concentric oil layer protected the encapsulated material by preventing exposure to the acidic environment of the stomach during digestion.
• A hydrogel core, unlike an aqueous core, provided high stability even under the high-osmolarity conditions of the stomach.
• Tuning the shell’s composition produced capsules that release selectively in response to the gut’s pH conditions.
• The system preserved the anti-inflammatory activities of 5-aminosalicylic acid (5-ASA) and Lys-Pro-Val (KPV) under stomach conditions and maintained their therapeutic effects on colonic epithelial cell migration and proliferation.

Relevance to KPV

This is a drug-delivery study in which KPV serves as one of two model anti-inflammatory payloads (alongside 5-ASA) validating an oral microsphere platform for IBD, rather than an investigation of KPV’s own pharmacology. Its relevance is practical: oral KPV faces the same gastric-degradation barrier this system is designed to overcome, and the demonstration that encapsulated KPV keeps its effect on colonic epithelial cell migration and proliferation supports formulation approaches for gut-targeted KPV. It complements other oral-delivery work on KPV for colitis, though the results here are in vitro proofs of concept, not efficacy data in animals or humans.

Citation

Jeong HS, Choi Y, Kim DW, et al. Multicompartmental Hydrogel Microspheres with a Concentric Thin Oil Layer: Protecting and Targeting Therapeutic Agents for Inflammatory Bowel Disease. ACS applied bio materials. 2025. doi:10.1021/acsabm.4c01763.

See Also

• Parent compound: KPV