New Chitosan Salt in Gastro-Resistant Oral Formulation Could Interfere with Enteric Bile Salts Emulsification of Diet Fats: Preliminary Laboratory Observations and Physiologic Rationale

Abstract

Chitosan (CH) is a polymer of glucosamine that is extracted from the shells of several sea fruits. It is well recognized as a nutritional supplement that is used to reduce body weight and blood lipid levels, but its clinical efficacy has not been clearly demonstrated. The true mechanism of action and physiological processes involved in these properties of CH are not yet understood or explained. The most accepted theories assume that CH reduces dietary fat absorption by trapping the fat in the gastric lumen. The very low pH of the gastric lumen induces CH jellification and, therefore, entrapment of the fats. This article describes the most plausible mechanism by which CH interferes with fat absorption in the first part of the enteric tract while interacting with cholic acids. We emphasize the weak points of the classic CH-containing formulations, which are unable to prove this theory. We also report preliminary experimental data of a new CH salt-containing formulation that is capable of effectively interfering with bile salt emulsification processes and, as a result, reducing dietary fat absorption.

Influence of Hydrocolloids (Dietary Fibers) on Lipid Digestion of Protein‐Stabilized Emulsions: Comparison of Neutral, Anionic, and Cationic Polysaccharides

“…The measured changes in particle charge can be attributed to a number of phenomena occurring within the simulated small intestine. First, the SSIF contain anionic bile salts that can interact with the cationic chitosan molecules through electrostatic interactions and form insoluble complexes (Thongngam and McClements , ; Fratter and others ). Second, the digestion of the lipid phase results in the formation of anionic free fatty acids that can also interact with the cationic chitosan molecules (Ylitalo and others ; Wydro and others ).…”

Effects of a New Nutraceutical Formulation (Berberine, Red Yeast Rice and Chitosan) on Non-HDL Cholesterol Levels in Individuals with Dyslipidemia: Results from a Randomized, Double Blind, Placebo-Controlled Study

“…Particularly, the acidic molecule selected to project this technology (PS) is a phosphorylated acid capable of cationizing CH and produce irreversible complexes with bile salts. The capability of coleosoma to entrap bile salts and the surrounding mechanism of action, have been investigated and proven in vitro [ 17 ].…”

“…Recently, a nutraceutical combination (red rice yeast extract (RRYE) titrated in monacolin (MC), berberine chloride (BC)), assembled in a new technology (named coleosoma) became commercially available (TegraDOC ® ). Briefly, it is composed of a gastro-resistant tablet containing, in the inner core, a chitosan (CH) polymer and an organic acid (phosphoserine, PS) that reduces enteric fat absorption [ 17 ]. This latter mechanism, coupled with the inhibition of HMG Co-A reductase and induced LDL-C clearance mediated by MC and BC, respectively, accounts for the lipid lowering properties of this compound.…”

<p>Osteochondral repair using scaffolds with gradient pore sizes constructed with silk fibroin, chitosan, and nano-hydroxyapatite</p>

“…31 Furthermore, CS also has antibacterial, anti-oxidant, and anti-tumor activities and has been widely used in biomedicine. [32][33][34] nHA is a bioactive ceramic with the chemical formula, [Ca 5 (OH)(PO 4 ) 3 ] x , that has a similar density to that of human teeth and bones. As an inorganic mineral, nHA has a typical apatite crystal structure and has similar inorganic components as the bone.…”