Controlling the Interaction between Starchy Polyelectrolyte Layers for Adjusting Protein Release from Nanocapsules in a Simulated Gastrointestinal Tract

Abstract

Orally delivered bioactive proteins face great challenges in the harsh environment of the upper gastrointestinal tract (GIT) in the field of functional foods based on bioactive proteins. Therefore, it is necessary to design carriers and delivery systems that have the potential to overcome the problem of lower bioaccessibility for protein cargoes. In this work, we present a starchy oral colon-targeting delivery system, capable of improving the release profile of the protein cargoes. The starchy oral colon-targeting delivery system was fabricated using layer-by-layer assembly of starchy polyelectrolytes (carboxymethyl anionic starch and spermine cationic starch) onto the surface of protein nanoparticles via electrostatic interaction. The dynamic change in the interaction between the starchy polyelectrolytes affected the shell aggregation structure and determined the release kinetics of nanocapsules in the GIT. Specifically, the stronger interactions between the starchy layers and the thicker and more compact shell layer kept the nanocapsule intact in the simulated gastric and intestinal fluids, better-protecting the protein from degradation by digestive fluids, thus avoiding the burst release effect in the SGF and SIF. However, the nanocapsule could quickly swell with the decreasing molecular interactions between starchy polyelectrolytes, increasing protein release (63.61%) in the simulated colonic fluid. Therefore, release behaviors of protein cargoes could be appropriately controlled by adjusting the number of deposited layers of pH-sensitive starchy polyelectrolytes on the nanocapsule. This could improve the bioaccessibility of oral targeted delivery of bioactive proteins to the colon.

Monascus Red Pigment Liposomes: Microstructural Characteristics, Stability, and Anticancer Activity

“…As shown in Figure 3c,d, the values of the exponent constant n of MRPs in SGF and SIF were 0.7451 and 0.6945, respectively, while those of MRPL were 1.0307 and 0.9096, respectively, which suggested that the release of MRPs in vitro was diffusion coupled with erosion, while that of MRPL was mainly erosion. Moreover, the K value of MRPL was smaller than that of MRPs, both in SGF and SIF, indicating that the release rate of MRPL was much slower due to the protective effect of liposome embedding [39]. 4a,b, MRPs and MRPL all exhibited inhibitory effects on the survival of MKN-28 and HepG-2 cells with a dose-dependent manner.…”

Surface Modification of Metallic Nanoparticles for Targeting Drugs

“…Metallic nanoparticles present opportunities to enhance central nervous system (CNS) drug delivery through strategies like functionalization with transcytosis ligands [10]. For example, intranasally administered fentanyl loaded in transferrin-conjugated nanoparticles exhibited rapid transport into the brain, providing prolonged pain relief in preclinical models [36]. The transferrin ligand enabled brain permeability by binding transferrin receptors onto nasal epithelial cells.…”

Delivery Systems to Enhance Bioaccessibility and Bioavailability of Bioactive Factors: Structure, Property, and Food Applications

“…Li et al fabricated a type of oral starchy colon-targeting delivery system, which could be used to improve the bioaccessibility of bioactive insulin. By using layer-by-layer assembly of starchy polyelectrolytes (carboxymethyl anionic starch and spermine cationic starch) onto the surface of insulin nanoparticles via electrostatic interaction, insulin nanoparticles could be protected from degradation by digestive fluids, thus avoiding their burst release in simulated gastric and intestinal fluids [ 2 ].…”