Targeted Gastrointestinal Delivery of Nutraceuticals with Polysaccharide‐Based Coatings

Abstract

Oral delivery is one of the facile methods for the administration of active ingredients (AIs) like nutraceuticals and drugs. However, its intrinsic disadvantages include poor absorption and bioavailability, degradation of the AI during transit through the gastrointestinal tract (GIT), and a lack of action specificity. Hence, a delivery system for targeted gastrointestinal delivery of AI using polysaccharide-based polymers, that are generally recognized as safe and approved for use as a direct food additive, is proposed. In this regard, mucoadhesive chitosan nanoparticles that could adhere to the mucosa of the GIT are fabricated and encapsulated with AI. These particles are subsequently coated with polysaccharides that have different enzymatic susceptibilities, to allow for specific degradation in the small or large intestines. It is observed that the polysaccharide coating efficiently retarded the nonspecific release of the encapsulated agent until it is exposed to its intended environment of release. The cytotoxicity and uptake of chitosan nanoparticles is further evaluated on Caco2 cells. In conclusion, these polysaccharide-coated nanoparticles can potentially be targeted to different organs in the GIT and to be taken up by the enterocytes for improved oral bioavailability.

Potential of Nanomaterial Applications in Dietary Supplements and Foods for Special Medical Purposes

“…Polysaccharides that have various enzymatic susceptibilities to ensure specific degradation in the small or large intestine when used as a NP coating can efficiently retard the nonspecific release of encapsulated bioactive compounds until the coating is exposed to its intended environment of release, and such coated NPs can be potentially targeted to different GI tract organs and taken up by the enterocytes, providing improved oral bioavailability [89].…”

Small-Intestine-Specific Delivery of Antidiabetic Extracts from Withania coagulans Using Polysaccharide-Based Enteric-Coated Nanoparticles

“…The chnp were designed in a way to be taken up by the enterocytes lining the small intestine to increase the bioavailability of the encapsulated compound. Having previously shown the uptake of chnp by Caco2 cells, 23 the release kinetics study evaluated the ability of the particles to release P4 inside the lysosome of the cells during the cell uptake. This was simulated using the pH 4.4 medium to mimic the condition inside the lysosome.…”

“…The fabrication and characterization of chitosan nanoparticles (chnp) and chnp coated with starch (C+S) were conducted similar to what had previously been reported by the authors. 23 Briefly, chnp were fabricated using electrospraying with the optimized parameters as follows: the concentration of chitosan dissolved in 50% acetic acid, 0.1% W/V; the concentration of TPP dissolved in water, 1% W/V with 0.5% (V/V) Tween 80; voltage, 25 kV; flow rate, 0.2 mL h –1 ; and working distance, 7 cm. The particles were electrosprayed directly into the cross-linking TPP solution and collected by centrifugation at an RCF of 13 000 g .…”

“…Release studies of P4 were carried out sequentially in simulated gastric fluid (SGF) (pH 1.2), simulated intestinal fluid (SIF) (pH 6.8), and pH 4.4 medium to mimic the path of the particles in the GIT. 23 Release studies were performed by suspending the particles in the release media at 37 °C in an incubator fitted with a rotating wheel at a speed of 20 rpm over a period of 48 h. The time frame in each simulated fluid was chosen to mimic the residence times of food in each region of the GIT: stomach (2 h), small intestine (3 h), and pH 4.4 buffer (PBS adjusted to pH 4.4) (43 h). At fixed time points, the medium was removed by centrifugation and replaced with fresh medium.…”

Self-Assembly of Amphiphilic Compounds as a Versatile Tool for Construction of Nanoscale Drug Carriers

“…Nanoparticles based on hydroxypropyl-β-CD and chitosan can be used in targeting various organs of the gastrointestinal tract. A study of the release of hydrophobic substrate from this composition showed a sharp release (more than 40%) in the gastric fluid due to the breakdown of chitosan and β-CD inclusion complex at low pH [ 261 ]. As in the case of hydrophilic substrate, only a small amount of hydrophobic substrate is released in the intestinal fluid.…”