<p>Stable oral delivery of macromolecules, which easily lose conformation and activity, is far more carrier-demanding than small molecules and a long-standing food science challenge. This study developed a cellulose-based IUSRHP to address this issue. Tests under separate independent conditions showed IUSRHP stayed stable in simulated gastric fluid (pH 3.0) for over 3&#xa0;h, and achieved unidirectional load release in simulated intestinal fluid (pH 7.2). Its loading capacity (96, 125, 200&#xa0;mg/piece at 10%, 30%, 50% sodium carboxymethylcellulose (NaCMC)) and thermal stability (glass transition temperature (Tg) from 219&#xa0;°C to 302&#xa0;°C) rose with NaCMC content. In the gastrointestinal tract, water permeated the pH-responsive layer, swelling the patch into a 3D hydrogel for unidirectional release of proteins (isoelectric point &lt; 7.2) (release rate tunable via protein negative charge). IUSRHP enhances local effective loads concentration, stability and bioavailability, key for stable oral delivery of food nutrient macromolecules or pharmaceutical active proteins.</p>

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Intestinal unidirectional sustained-release hydrogel patch designed for stable oral delivery of active nutrient macromolecules based on pH response

  • Minquan Xia,
  • Zhengfeng Fang,
  • Lu Wang,
  • Yi Wang,
  • Yan Zhu,
  • Tao Zeng,
  • LiZhi Lu,
  • Zhaoxia Cai

摘要

Stable oral delivery of macromolecules, which easily lose conformation and activity, is far more carrier-demanding than small molecules and a long-standing food science challenge. This study developed a cellulose-based IUSRHP to address this issue. Tests under separate independent conditions showed IUSRHP stayed stable in simulated gastric fluid (pH 3.0) for over 3 h, and achieved unidirectional load release in simulated intestinal fluid (pH 7.2). Its loading capacity (96, 125, 200 mg/piece at 10%, 30%, 50% sodium carboxymethylcellulose (NaCMC)) and thermal stability (glass transition temperature (Tg) from 219 °C to 302 °C) rose with NaCMC content. In the gastrointestinal tract, water permeated the pH-responsive layer, swelling the patch into a 3D hydrogel for unidirectional release of proteins (isoelectric point < 7.2) (release rate tunable via protein negative charge). IUSRHP enhances local effective loads concentration, stability and bioavailability, key for stable oral delivery of food nutrient macromolecules or pharmaceutical active proteins.