Hierarchically structured phase separated biopolymer hydrogels create tailorable delayed burst release during...

Area of Science:

• Biotechnology
• Materials Science
• Pharmaceutical Sciences

Background:

• Oral delivery of active pharmaceutical ingredients (APIs) faces challenges due to degradation in the gastrointestinal tract.
• Biodegradable biopolymer hydrogels offer potential for controlled release but require optimization for specific actives like lipids.

Purpose of the Study:

• To develop novel hierarchical biopolymer hydrogels for controlled release of lipids/lipophilic APIs.
• To mathematically model the release mechanisms and program the release timing.

Main Methods:

• Creation of core-shell hydrogels with phase-separated protein/polysaccharide cores and mixed biopolymer shells.
• Utilizing gelatin, oil-in-water emulsion, xanthan, and β-lactoglobulin for hydrogel fabrication.
• Investigating enzyme mass transport and surface erosion as degradation mechanisms.

Main Results:

• The core-shell structure enabled a tailorable delayed burst release of APIs during simulated gastrointestinal digestion.
• Release delay (60-240 min) was programmable by adjusting shell thickness or protein concentration (70-140 µg/L β-lactoglobulin).
• A kinetic model accurately predicted the influence of shell properties on in vitro gastrointestinal release timing.

Conclusions:

• A novel family of core-shell hydrogel oral dosage forms for programmable delivery of lipids/lipophilic APIs was created.
• These hydrogels demonstrate potential for improved delivery of peptides, poorly soluble drugs, and lipids in the GI tract.