pH-Responsive Nanocolloids for Oral Drug Delivery Show Promise

Researchers at the University of Queensland have developed a novel pH-responsive nanocolloid system for oral drug delivery, which has shown to improve the solubility, dissolution, and permeability of poorly soluble nutraceuticals in the gastrointestinal tract. The study utilized natural compounds such as bovine beta-lactoglobulin (BLG) and succinylated beta-lactoglobulin (succ. BLG) cross-linked with epsilon poly-L-lysine (BCEP and BCP) to create colloids with high loading capacity and aqueous solubility. These nanocomplexes were capable of encapsulating curcumin with high encapsulation efficiency and sustained release in the small intestine.

Key Takeaways:

  • The pH-responsive nanocolloid system was developed using natural compounds such as bovine beta-lactoglobulin (BLG) and succinylated beta-lactoglobulin (succ. BLG) cross-linked with epsilon poly-L-lysine (BCEP and BCP).
  • The colloids had a diameter of around 200 nm and were capable of encapsulating curcumin with ~100% encapsulation efficiency and ~10% w/w drug loading.
  • Cross-linking succ. BLG with E-PLL significantly enhanced curcumin's permeability in an in-vitro Caco-2 cell monolayer model compared to curcumin solution or non-crosslinked BLG/succ.
  • The nanocomplexes reduced the production of inflammatory cytokines and chemokines such as Tnfa and Cxcl10 more than curcumin solution or suspension, while being non-toxic to organoids.
  • The research concluded that the pH-responsive nanocolloid system has the potential to improve the solubility, dissolution, and permeability of poorly soluble nutraceuticals in the gastrointestinal tract, and is a promising tool for oral drug delivery.
  • The study suggests that the use of natural compounds and pH-responsive nanocolloids could revolutionize the field of drug delivery, providing a more efficient and effective way to deliver medications.

Statistics:

  • 200 nm: the diameter of the pH-responsive nanocolloids.
  • ~100%: the encapsulation efficiency of curcumin in the nanocomplexes.
  • ~10% w/w: the drug loading of curcumin in the nanocomplexes.
  • ~160-fold: the increase in aqueous solubility of curcumin when formed with BLG.
  • ~86-fold: the increase in aqueous solubility of curcumin when formed with succ. BLG.
  • 1% DMSO: the concentration of curcumin solution used as a control in the in-vitro Caco-2 cell monolayer model.
  • 7.4: the pH of the small intestine, where the sustained release of curcumin was observed.
  • 10.1016/j.jcis.2020.12.054: the direct object identifier (DOI) for the research article.

Sources:

  • "pH - Responsive colloidal carriers assembled from b-lactoglobulin and Epsilon poly-L-lysine for oral drug delivery." Journal of Colloid and Interface Science, vol. 589, 2020, pp. 45-55.
  • Journal of Colloid and Interface Science, Elsevier, 525 B St, Ste 1900, San Diego, CA 92101-4495, USA.
  • Rabina Giri, Faculty of Medicine, University of Queensland, Brisbane, QLD 4072, Australia.
  • DOI: 10.1016/j.jcis.2020.12.054.