Citrus peel pectin and alginate-based emulgel particles for small intestine-targeted oral delivery of curcumin.

Polysaccharides are a prominent choice in the realm of food-grade oral delivery systems due to their resistance to degradation by digestive enzymes in the oral, gastric, and small intestinal environments, as well as their ease of production, cost-effectiveness, and potential health benefits as prebiotics. Furthermore, their ability to respond to pH-induced dissolution, along with their emulsifying properties, can be strategically employed to achieve precise targeting of lipophilic bioactives to the small intestine. In this study, citrus peel pectin and alginate served as stabilizers for emulgel particles without supplementary emulsifiers or gelling agents. Within this system, pectin functioned as an emulsifier, while alginate acted as a gelling agent, facilitated by Ca2+-induced ionic crosslinking. The synergistic interplay between pectin and alginate efficiently protected curcumin in gastric conditions and controlled dissolution in the small intestine, depending on the pectin/alginate ratio. These controlled phenomena facilitated lipolysis, curcumin release, and ultimately enhanced curcumin bioaccessibility. Furthermore, once the emulgel particle released all the entrapped curcumin in the small intestine, residual polysaccharides underwent facile degradation by pectinase and alginate lyase, yielding fermentable monosaccharides. This confirms the potential of the emulgel particles for use as a prebiotic in the colon. These findings offer significant promise for enhancing the systematic design of food-grade delivery systems that encapsulate lipophilic bioactives, achieving controlled release, enhanced stability, and improved bioaccessibility. Importantly, this system can comprise components that undergo complete digestion, absorption, and utilization in the human body, encompassing materials such as oil, nutraceuticals, and prebiotics, all without presenting health risks.

PH sensitive double-layered emulsions stabilized by bacterial cellulose nanofibers/soy protein isolate/chitosan complex enhanced the bioaccessibility of curcumin: In vitro study.

In this work, double-layered emulsions stabilized by bacterial cellulose nanofibers/soy protein isolate/chitosan complex were prepared using layer-by-layer self-assembly technology and used for the delivery of curcumin, and the physical and delivery properties of the prepared double-layered emulsions were investigated. The zeta-(ζ) potential of colloidal particles confirmed that the chitosan was adsorbed on surface of the single-layered emulsion droplets by attractive electrostatic interactions. Meanwhile, the physical properties showed that the double-layered emulsions displayed high pH-sensitivity and showed relatively higher stability under acid environment. Furthermore, the in vitro digestion result showed that the curcumin loaded by double-layered emulsions were more stable during simulated gastric digestion as compared with that loaded by single-layered emulsions. Especially, the bioaccessibility of curcumin delivered by the double-layered emulsions (77.4 ± 3.25%) was significantly higher than that of curcumin delivered by single-layered emulsions (32.8 ± 2.56%). Therefore, it can be concluded that the prepared double-layered emulsions showed a great potential application in the delivery of fat-soluble bioactive compounds.

In vitro evaluation of the gastrointestinal delivery of acid-sensitive pancrelipase in a next generation enteric capsule using an exocrine pancreatic insufficiency disease model.

The dissolution characteristics of five capsules (Next Generation Enteric [NGE], Vcaps® Enteric [VCE], VCE DUOCAP® [VCE/VCE] system, Hard Gelatin Capsule [HGC] as negative control, and Creon® 10,000 U as market reference) were evaluated using an in vitro simulation of the stomach and upper intestinal tract with an acidic duodenal incubation (pH 4.5 for the first 10 min, pH 6 for the remaining 17 min) to simulate exocrine pancreatic insufficiency. Caffeine was a marker of capsule dissolution, and tributyrin to butyrate conversion measured pancrelipase activity. All capsules were filled with pancrelipase; the NGE, VCE, VCE/VCE, and HGC capsules also contained 50 mg caffeine. Caffeine was released first from the HGC capsule, followed by the VCE, NGE, and VCE/VCE capsules. Pancrelipase activity followed this trend and demonstrated a similar activity level over time for the NGE, VCE/VCE, and Creon® capsules. The HGC formulation confirmed gastric degradation of unprotected pancrelipase. NGE capsules provided similar protection to the simple fill formulation as observed for the complex formulation of the Creon® capsule in a setting with increased pepsin activity and may hasten the time needed to go from formula development to first-in-human studies for pH sensitive drugs or those requiring small intestine targeting.

Preparation and Characterization of Beads of Sodium Alginate/Carboxymethyl Chitosan/Cellulose Nanofiber Containing Porous Starch Embedded with Gallic Acid: An In Vitro Simulation Delivery Study.

In this study, a system was designed that can encapsulate and deliver gallic acid (GA), which was composed of polysaccharide polymers based on sodium alginate (SA), carboxymethyl chitosan (CCT), and cellulose nanofibers (CN) and was assisted by porous starch. The compositions were characterized by rheology and zeta potentials, and the results showed that the materials used in this study could effectively guarantee the stability of the system. The morphology and chemical structure of the beads were characterized by SEM and FT-IR, the results indicated that the addition of CCT could effectively reduce the cracks and pores on the surface of the beads, which was beneficial to the encapsulation and delivery of GA. Moreover, the results of the swelling rate, release tests, and antioxidant tests also proved the effectiveness of the system. The pH response effect of SA/CN/CCT (SCC) beads and the protection of GA were superior, and the release rate of GA in simulated gastric fluid (SGF) was only 6.95%, while SA and SA/CN (SCN) beads reached 57.94% and 78.49%, respectively. In conclusion, the interpenetrating network polymers constructed by SA, CCT, and CN, which, combined with porous starch as a coating layer, can achieve the embedding and the delivery of GA.