Microencapsulation of Ionic Liquid by Interfacial Self-Assembly of Metal-Phenolic Network for Efficient Gastric Absorption of Oral Drug Delivery

Abstract

Improving bioavailability of orally delivered drugs is still challenging, as conventional drug delivery systems suffer from non-specific drug delivery in the gastrointestinal (GI) tract and limited drug absorption efficiency. Gastric drug delivery is even more difficult due to the harsh microenvironment, short retention time, and physiologic barriers in the stomach. Here, an oral drug delivery microcapsule system was developed for gastric drug delivery, which consists of ionic liquid (IL) as the inner carrier and metal-phenolic network (MPN) as the microcapsule shell. The IL@MPN microcapsules are prepared by interfacial self-assembly of Fe III and quercetin at the interface of hydrophobic IL ([EMIM][NTf 2 ]) and water. The formation of MPN shell could improve the stability of IL droplets in water and endow the system with pH-response drug release properties, while the encapsulated IL core could efficiently load the drug and enhance the drug tissue permeability. The IL@MPN microcapsules showed enhanced drug absorption in the stomach after oral administration in a rat model, where the microcapsules are disassembled in gastric acid, and the released IL could reduce the viscosity of mucus gel and increase the drug transport rate across endothelial cells. This work presents a simple yet efficient strategy for oral drug delivery to the stomach. Given the diversity and versatility of both MPN and IL, the proposed self-assembled microcapsules could expand the toolbox of drug delivery systems with enhanced oral drug bioavailability.

Bi-functional quercetin/copper nanoparticles integrating bactericidal and anti-quorum sensing properties for preventing the formation of biofilms

“…32 Similar to other phenolic–metal complexes, the QC complex also exhibited pH sensitivity. 33–35 As shown in Fig. 1e, the overall release of Cu 2+ ions from the QC NPs was greater at pH 5.0 than at pH 7.4 at the specified timepoint, which suggests that the QC complex could undergo dissociation to release Cu 2+ ions and Qe in a mildly acidic environment.…”

Ionic liquids revolutionizing biomedicine: recent advances and emerging opportunities

“…8D). 264 Zhou et al used poly(lactide- co -glycolide) as the backbone, choline arginine for protein protection, and vitamin B12-chitosan for mucosal adhesion and pH responsiveness. 278 Choline arginine proved effective in maintaining insulin stability throughout delivery system preparation, transportation, and storage.…”

In Situ Gelation Strategy for Efficient Drug Delivery in a Gastrointestinal System

“…These excellent properties highlight the immense potential of MPN coatings as biocompatible capsule membranes (microcapsules). 36 Besides being physically adsorbed onto solid substrates (e.g., organic and inorganic materials) for prolonged retention in the GI tract, MPNs can assemble at liquid−liquid interfaces (e.g., water/oil microemulsions) to suspend drug release in gastric fluids over an extended period. Recent studies have discovered that, after complete solidification of the capsule shell, solvent extraction within microcapsules induces gasification, resulting in gas-filled microcapsules with uniform particle size, slow degradation rates, and strong long-term suspension capabilities.…”