Core–Shell Biopolymer Nanoparticles for Co-Delivery of Curcumin and Piperine: Sequential Electrostatic Deposition of Hyaluronic Acid and Chitosan Shells on the Zein Core

Abstract

Curcumin and piperine are natural nutraceuticals that exhibit synergistic biological activities, but have different polarities, which can make their encapsulation within a single delivery system challenging. In this study, the two bioactive components were encapsulated within core–shell nanoparticles formed by a combination of antisolvent precipitation and layer-by-layer deposition. Initially, strongly hydrophobic curcumin (log P = 4.12) was embedded in the hydrophobic core of zein-hyaluronic acid nanoparticles using the antisolvent precipitation method. Then, the weakly hydrophobic piperine (log P = 2.78) was adsorbed to the outer biopolymer shell of these nanoparticles. Finally, the nutraceutical-loaded particles were coated with a layer of chitosan by the electrostatic deposition method. The surface charge and coating thickness depended on the number of adsorbed layers and the nature of the outer layer, being negative for hyaluronic acid and positive for chitosan. Low-, medium-, and high-molecular weight chitosan were utilized to modify the surface properties. Chitosan with a low-molecular weight was selected to fabricate the core–shell nanoparticles because it produced small highly charged cationic particles (d = 599 nm; ζ = +38.1 mV). The encapsulation efficiency and loading capacities were 90.4 and 5.7% for curcumin, and 86.4 and 5.4% for piperine, respectively. The core–shell nanoparticles protected the nutraceuticals from chemical degradation during light exposure, thermal processing, and storage for 2 months. Moreover, the nanoparticles were able to control the release of the bioactive components in simulated gastrointestinal conditions. Our results should facilitate the development of more effective nanodelivery systems for nutraceuticals that exhibit synergistic activities, but have different molecular characteristics.

Oral Core–Shell Nanoparticles Embedded in Hydrogel Microspheres for the Efficient Site-Specific Delivery of Magnolol and Enhanced Antiulcerative Colitis Therapy

“…In Mag@CS-Zein NPs, the characteristic peak of free Mag was completely covered, which proved that Mag was successfully encapsulated into NPs. 36 XRD can be used to evaluate the change of the crystal form of the material so as to investigate the physical loading properties of the NPs. As shown in Figure 1E, there were some sharp peaks at 11.3, 13.3, 15.2, 19.9, 21.8, 23.1, and 26.3°in free Mag, suggesting that pure nutraceuticals were in the crystalline state.…”

Precision and Advanced Nano-Phytopharmaceuticals for Therapeutic Applications

“…Multi-compound bioactive complexes like curcumin-piperine are challenging to create, due to their distinct polarities. To overcome this, the two components were encased in core-shell NPs through antisolvent precipitation and progressive layering of zein-hyaluronic acid, followed by chitosan coating [41].…”

Endocytosis of abiotic nanomaterials and nanobiovectors: Inhibition of membrane trafficking

“…Different approaches may be used to modulate the elasticity of such particles, including controlling the materials used in the layers, the number of layers, the density of layer crosslinking, and removing the core of the capsules [164] . For example, core-shell particles that consist of a solid polymeric core inside a lipid shell with cylindrical polymer brushes exhibited excellent elasticity [165] , [166] , [167] . Layer-by-layer capsules synthesized using a silica template exhibited increased stiffness values after replacement of the core with Au nanoparticles [168] .…”