Anticancer and Antibacterial Properties of Curcumin-Loaded Mannosylated Solid Lipid Nanoparticles for the Treatment of Lung Diseases.

Lung cancer and Mycobacterium avium complex infection are lung diseases associated with high incidence and mortality rates. Most conventional anticancer drugs and antibiotics have certain limitations, including high drug resistance rates and adverse effects. Herein, we aimed to synthesize mannose surface-modified solid lipid nanoparticles (SLNs) loaded with curcumin (Man-CUR SLN) for the effective treatment of lung disease. The synthesized Man-CUR SLNs were analyzed using various instrumental techniques for structural and physicochemical characterization. Loading curcumin into SLNs improved the encapsulation efficiency and drug release capacity, as demonstrated by high-performance liquid chromatography analysis. Furthermore, we characterized the anticancer effect of curcumin using the A549 lung cancer cell line. Cells treated with Man-CUR SLN exhibited an increased cellular uptake and cytotoxicity. Moreover, treatment with free CUR could more effectively reduce cancer migration than treatment with Man-CUR SLNs. Similarly, free curcumin elicited a stronger apoptosis-inducing effect than that of Man-CUR SLNs, as demonstrated by reverse transcription-quantitative PCR analysis. Finally, we examined the antibacterial effects of free curcumin and Man-CUR SLNs against Mycobacterium intracellulare (M.i.) and M.i.-infected macrophages, revealing that Man-CUR SLNs exerted the strongest antibacterial effect. Collectively, these findings indicate that mannose-receptor-targeted curcumin delivery using lipid nanoparticles could be effective in treating lung diseases. Accordingly, this drug delivery system can be used to target a variety of cancers and immune cells.

Influence of carboxymethyl cellulose on the stability, rheology, and curcumin bioaccessibility of high internal phase Pickering emulsions.

Recently, there has been a focus on using biopolymer-based particles to stabilize high internal phase Pickering emulsions (HIPPEs) due to the notable advances in biocompatibility and biodegradability. In this work, the complex particles of peanut protein isolate and carboxymethyl cellulose (CMC) with various substitution degrees (DS; 0.7 and 0.9) and weight average molecular weights (Mw; 90, 250, and 700 kDa) were prepared and characterized as novel stabilizers. For the obtained four types of morphologically distinct particles, the complex particles formed by CMC (0.9 DS and 250 kDa) showed cluster structures with an average size of 1.271 µm, equally biphasic wettability with three-phase contact angles of 91.5°, and the highest diffusion rate at the oil-water interface. HIPPEs stabilized by these particles exhibited more elastic behavior due to the smaller tanδ and higher viscosity, as well as excellent thixotropic recovery properties and stability against heating, storage, and freeze-thawing. Furthermore, confocal laser scanning microscopy verified that these particles formed a dense interfacial layer around the oil droplets, which could resist flocculation and coalescence between oil droplets during in vitro digestion. The improved bioaccessibility of curcumin-loaded HIPPEs made these delivery systems potentially apply in functional foods.

Discovery of cinnamylaldehyde-derived mono-carbonyl curcumin analogs as anti-gastric cancer agents via suppression of STAT3 and AKT pathway.

The structural modification of curcumin has always been a hotspot in drug development. In this paper, a class of cinnamylaldehyde-derived mono-carbonyl curcumin analogs (MCAs) with 7-carbon-links were designed and synthesized and their anticancer properties were evaluated. Through screening anti-gastric cancer activity of these compounds, H1 exhibited the strongest cytotoxic activity by inhibiting cell viability and colony formation, inducing cell cycle G2/M phase arrest in vitro (SGC-7901 and AGS gastric cancer cells). Moreover, the SGC-7901 subcutaneous tumor-bearing mice studies revealed that H1 significantly inhibited the tumor growth of gastric cancer. We explored the possible potential targets of H1 through network pharmacology. Mechanistically, our results demonstrated that H1 showed potential anti-gastric cancer activity through suppression of the STAT3 and AKT signaling pathway in vitro and in vivo, which was validated by molecular docking. Overall, our results indicate the potential of H1 as a potent chemotherapeutic drug against gastric cancer.

Porous corn starch granules as effective host matrices for encapsulation and sustained release of curcumin and resveratrol.

Type 2 Diabetes Mellitus (T2DM) is a carbohydrate-rich diet-regulated ailment with carbohydrates digested and absorbed rapidly. Hence, modulating carbohydrate digestion is warranted; to this end, polyphenols from plant sources are handy. However, polyphenols' instability and low bioavailability limit their wholesome use, and thus, encapsulating them into an inexpensive and suitable wall material would be the best strategy. Herein, the potential of porous starch granules is demonstrated. Curcumin and resveratrol were chosen as the test polyphenols due to their proven health benefits, and porous corn starch granules were chosen as the wall material. Porous corn starch granules were prepared through enzymatic modification with 11, 22, and 33 units of amyloglucosidase at three reaction times of 2, 4, and 6 h. The polyphenols were loaded at 100, 200, and 500 mg concentrations in 1 g of starch for 21 days and were characterized through Scanning Electron Microscope (SEM) and Fourier Transform Infrared spectroscopy (FTIR) analyses. The encapsulation efficiency was determined, the rate of starch digestion was calculated through the Englyst test, and polyphenols' in vitro release behavior in gastric and intestinal fluids was measured. Results suggest that 33 enzyme units for a 2 h reaction time were optimal for forming spherical-oval pores on corn starch granules with the maximum encapsulation efficiency of 80.16 % and 88.33 % for curcumin and resveratrol, respectively. The FTIR results suggest the entrapment of polyphenols inside the starch matrix. The inclusion significantly reduced starch digestion and increased the percentage of resistant starch up to 41.11 % and 66.36 % with curcumin and resveratrol, respectively. The in vitro release behavior demonstrated good stability in the simulated gastric fluids and sustained release in simulated intestinal fluids. The encapsulated polyphenols showed a complex Fickian type of diffusion mechanism. Overall, the results suggest that porous corn starch granules could be a potential delivery system for curcumin and resveratrol and will aid in developing novel functional foods to address the T2DM concerns.

Curcumin encapsulated in milk small extracellular vesicles as a nanotherapeutic alternative in experimental chronic liver disease.

Curcumin is a natural molecule widely tested in preclinical and clinical studies due to its antioxidant and anti-inflammatory activity. Nevertheless, its high hydrophobicity and low bioavailability limit in vivo applications. To overcome curcumin´s drawbacks, small extracellular vesicles (sEVs) have emerged as potential drug delivery systems due to their non-immunogenicity, nanometric size and amphiphilic composition. This work presents curcumin cargo into milk sEV structure and further in vitro and in vivo evaluation as a therapeutic nanoplatform. The encapsulation of curcumin into sEV was performed by two methodologies under physiological conditions: a passive incorporation and active cargo employing saponin. Loaded sEVs (sEVCurPas and sEVCurAc) were fully characterized by physicochemical techniques, confirming that neither methodology affects the morphology or size of the nanoparticles (sEV: 113.3±5.1 nm, sEVCurPas: 127.0±4.5 nm and sEVCurAc: 98.5±3.6 nm). Through the active approach with saponin (sEVCurAc), a three-fold higher cargo was obtained (433.5 µg/mL) in comparison with the passive approach (129.1 µg/mL). These sEVCurAc were further evaluated in vitro by metabolic activity assay (MTT), confocal microscopy, and flow cytometry, showing a higher cytotoxic effect in the tumoral cells RAW264.7 and HepG2 than in primary hepatocytes, specially at high doses of sEVCurAc (4%, 15% and 30% of viability). In vivo evaluation in an experimental model of liver fibrosis confirmed sEVCurAc therapeutic effects, leading to a significant decrease of serum markers of liver damage (ALT) (557 U/L to 338 U/L with sEVCurAc therapy) and a tendency towards decreased liver fibrogenesis and extracellular matrix (ECM) deposition.

Construction, characterization and bioactivity evaluation of curcumin nanocrystals with extremely high solubility and dispersion prepared by ultrasound-assisted method.

Curcumin (Cur) as a natural pigment and biological component, can be widely used in food and beverages. However, the water insolubility of Cur significantly limits its applications. In this study, we prepared a series of nanocrystals via ultrasound-assisted method to improve the solubility and availability of Cur. The results showed artemisia sphaerocephala krasch polysaccharide (ASKP), gum arabic (GA) and wheat protein (WP) were outstanding stabilizers for nanocryatals except traditional agent, poloxamer 188 (F68). The obtained curcumin nanocrystals (Cur-NC) displayed a rod-shaped, crystal- and nanosized structure, and extremely high loading capacity (more over 80 %, w/w). Compared with raw powder, Cur-NC greatly improved the water solubility and dispersibility, and the slow and complete release of Cur of Cur-NC also endowed them excellent antioxidant capacities even at 10 µg/mL. Importantly, as functional factor additive in beverages (e.g. water and emulsion), Cur-NC could increase the content of Cur to at least 600 µg/mL and retain a good stability. Overall, we provided an effective improvement method for the liposoluble active molecules (e.g. Cur) based on the nanocrystals, which not only tremendously enhanced its water solubility, but also strengthened its bioactivity. Notably, our findings broadened the application of water-insoluble compounds.

Preparation and application of curcumin loaded with citric acid crosslinked chitosan-gelatin hydrogels.

While oral administration offers safety benefits, its therapeutic efficacy is hindered by various physiological factors within the body. In this study, a novel approach was explored using a matrix consisting of 2 % chitosan and 2 % gelatin, with citric acid (CA) serving as a green cross-linking agent (ranging from 0.4 % to 1.0 %), and curcumin (Cur) as the model drug to formulate hydrogel carriers. The results showed that a 0.4 % CA concentration, the hydrogel (CGA0.4) reached swelling equilibrium in deionized water within 40 min, exhibiting a maximum swelling index was 539 g/g. The addition of Cur to the CGA hydrogel (CGACur) notably enhanced release efficiency, particularly in simulated intestinal fluid, where Cur release rates exceeded 40 % within 100 min compared to below 8 % in other solutions. Among these hydrogels, CGA0.4Cur exhibited the fastest degradation rate in the combined solution, reaching >90 % degradation after 7 days. Additionally, Cur and CA demonstrated positive effects on the tensile strength, antioxidant activity and antibacterial activity of hydrogels. Compare to the bioaccessibility of CGC (27 %), those of CGACur had increased to over 34 %. These findings offer provide theoretical support for CA-crosslinked chitosan/gelatin gels in delivering hydrophobic bioactive molecules and their application in intestinal drug delivery system.

Preparation, stability, and antibacterial activity of carboxymethylated Anemarrhena asphodeloides polysaccharide-chitosan nanoparticles loaded curcumin.

In present study, polysaccharide polyelectrolyte nanoparticles (CMAAP-CS NPs) were constructed by mixing carboxymethylated Anemarrhena asphodeloides polysaccharide (CMAAP) and chitosan (CS). CMAAP-CS NPs were applied as carrier to improve the bioavailability and stability of curcumin (Cur). The average particle size of CMAAP-CS NPs was 216.60 ± 4.21 nm and the entrapment efficiency of Cur reached 82.50 ± 2.09 %. The simulated digestion experiments in vitro confirmed that the bioavailability of Cur loaded in CMAAP-CS NPs was 59.84 ± 0.03 % after saliva, gastric and intestinal digestion, which was obvious higher than 21.57 ± 0.07 % of free Cur under the same conditions. The results of stability testing revealed that CMAAP-CS NPs could markedly reduce the degradation of Cur against storage, heating, UV light treatment, and neutral pH. This study provided promising polyelectrolyte complex loaded hydrophobic nutrients in medicine industry.

Preparation, characterization, and ex-vivo evaluation of curcumin-loaded niosomal nanoparticles on the equine sperm quality during cooled storage.

Oxidative damage to sperm during cooled storage is a significant issue, and curcumin, with its antioxidant properties, could be a solution. However, its low bioavailability presents a challenge that this study aims to address. The primary objective of this study was to investigate the potential of curcumin-loaded niosomal nanoparticles (Cur-LNN) to enhance the antioxidant properties of curcumin and its effect on sperm quality during 72 h cooled storage. The thin-film hydration procedure was applied to prepare Cur-LNN. The fabricated noisomal nanocarriers were characterized using dynamic light scattering (DLS), transmission electron microscopy (TEM), field emission scanning electron microscopy (FESEM), and Fourier-transform infrared (FT-IR) spectroscopy. Moreover, the encapsulation and loading efficiency, in vitro release study, and ex-vivo antioxidant functionality of Cur-LNN on the stallion sperm preserved under cooled storage conditions were assessed. The fabricated Cur-LNN was spherical in shape and had an average particle size of 163.1 ± 1.8 nm, a zeta potential of -34.1 ± 1.9 mV, a poly-dispersity index of 0.339 ± 0.045, an encapsulation efficiency of 92.34 ± 0.18 %, and a loading efficiency of 35.57 ± 1.36 %. Ex-vivo evaluation revealed that supplementation of the semen extender with Cur-LNN has the potential to enhance sperm quality by improving total and progressive motility, plasma membrane functionality, and lipid peroxidation. These results demonstrate that Cur-LNN exhibited stronger antioxidant and protective effects than curcumin. Although further in vivo investigations are warranted, our ex-vivo results suggest that Cur-LNN has the potential to attenuate oxidative damage and can be used to fortify the antioxidant capacity of equine semen under cooled storage conditions.

Curcumin/TGF-ß1 siRNA loaded solid lipid nanoparticles alleviate cerebral injury after intracerebral hemorrhage by transnasal brain targeting.

Intracerebral hemorrhage (ICH) is a prevalent cerebrovascular disorder. The inflammation induced by cerebral hemorrhage plays a crucial role in the secondary injury of ICH and often accompanied by a poor prognosis, leading to disease exacerbation. However, blood-brain barrier (BBB) limiting the penetration of therapeutic drugs to the brain. In this paper, our primary objective is to develop an innovative, non-invasive, safe, and targeted formulation. This novel approach aims to synergistically harness the combined therapeutic effects of drugs to intervene in inflammation via a non-injectable route, thereby significantly mitigating the secondary damage precipitated by inflammation following ICH. Thus, a novel "anti-inflammatory" cationic solid lipid nanoparticles (SLN) with targeting ability were constructed, which can enhance the stability of curcumin(CUR) and siRNA. We successfully developed SLN loaded with TGF-ß1 siRNA and CUR (siRNA/CUR@SLN) that adhere to the requirements of drug delivery system by transnasal brain targeting. Through the characterization of nanoparticle properties, cytotoxicity assessment, in vitro pharmacological evaluation, and brain-targeting evaluation after nasal administration, siRNA/CUR@SLN exhibited a nearly spherical structure with a particle size of 125.0±1.93 nm, low cytotoxicity, high drug loading capacity, good sustained release function and good stability. In vitro anti-inflammatory results showcasing its remarkable anti-inflammatory activity. Moreover, in vivo pharmacological studies revealed that siRNA/CUR@SLN can be successfully delivered to brain tissue. Furthermore, it also elicited an effective anti-inflammatory response, alleviating brain inflammation. These results indicated that favorable brain-targeting ability and anti-inflammatory effects of siRNA/CUR@SLN in ICH model mice. In conclusion, our designed siRNA/CUR@SLN showed good brain targeting and anti-inflammatory effect ability after nasal administration, which lays the foundation for the treatment of inflammation caused by ICH and offers a novel approach for brain-targeted drug delivery and brings new hope.

Fabrication and characterization of curcumin-loaded composite nanoparticles based on high-hydrostatic-pressure-treated zein and pectin: Interaction mechanism, stability, and bioaccessibility.

We successfully designed curcumin (Cur)-loaded composite nanoparticles consisting of high-hydrostatic-pressure-treated (HHP-treated) zein and pectin with a pressure of 150 MPa (zein-150 MPa-P-Cur), showing nano-spherical structure with high zeta-potential (-36.72 ± 1.14 mV) and encapsulation efficiency (95.64 ± 1.23 %). We investigated the interaction mechanism of the components in zein-150 MPa-P-Cur using fluorescence spectroscopy, molecular dynamics simulation, Fourier-transform infrared spectrometry and scanning electron microscopy techniques. Compared with zein-P-Cur, the binding sites and binding energy (-53.68 kcal/mol vs. - 44.22 kcal/mol) of HHP-treated zein and Cur were increased. Meanwhile, the interaction force among HHP-treated zein, pectin, and Cur was significantly enhanced, which formed a tighter and more stable particle structure to further improve package performance. Additionally, Cur showed the best chemical stability in zein-150 MPa-P-Cur. And the bioavailability of Cur was increased to 65.53 ± 1.70 %. Collectively, composite nanoparticles based on HHP-treated zein and pectin could be used as a promising Cur delivery system.

Ultra-stable pickering emulsion stabilized by anisotropic pea protein isolate-fucoidan conjugate particles through Maillard reaction.

Bio-based emulsifiers hold significant importance in various industries, particularly in food, cosmetics, pharmaceuticals and other related fields. In this study, pea protein isolate (PPI) and fucoidan (FUD) were conjugated via the Maillard reaction, which is considered safe and widely used in the preparation of food particle. The PPI-FUD conjugated particles exhibit an anisotropic non-spherical structure, thereby possessing a high detachment energy capable of preventing emulsion coalescence and Ostwald ripening. Compared to emulsions previously prepared in other studies (< 500 mM), the Pickering emulsion stabilized by PPI-FUD conjugate particles demonstrates outstanding ionic strength resistance (up to 5000 mM). Furthermore, when encapsulating curcumin, the Pickering emulsion protects the curcumin from oxidation. Additionally, the formulated emulsions demonstrated the capability to incorporate up to 60 % (v/v) oil phase, revealing remarkable performance in terms of storage stability, pH stability, and thermal stability.

Phyto-cosmeceutical gel containing curcumin and quercetin loaded mixed micelles for improved anti-oxidant and photoprotective activity.

Ultra Violet radiations induced skin damage and associated skin disorders are a widespread concern. The consequences of sun exposure include a plethora of dermal conditions like aging, solar urticaria, albinism and cancer. Sunscreens provide effective protection to skin from these damages. Besides FDA approved physical and chemical UV filters, phytoconstituents with their multi functionalities are emerging as frontrunners in Therapy of skin disorders. Objective of this study was to develop novel phyto-dermal gel (PDG) with dual action of sun protection and antioxidant potential using polymeric mixed micelles (PMMs) are nanocarriers. PMMs of Pluronic F127 and Pluronic F68 loaded with curcumin and quercetin were optimized by 32 factorial designs. Responses studied were vesicle size, SPF, entrapment efficiency of curcumin and quercetin and antioxidant activity. Droplet size ranged from 300 to 500 nm with PDI in between 0.248 and 0.584. Combination of curcumin and quercetin showed enhanced sun protection and antioxidant activity. Pluronics played a significant positive role in various parameters. In present studies vesicle size of factorial batches was found to be between 387 and 527 nm, and SPF was found to be between 18.86 and 28.32. Transmission electron microscopy revealed spherical morphology of micelles. Optimized micelles were incorporated into Carbopol 940. Optimized PDG was evaluated for pH, drug content, spreadability, rheology, syneresis, ex vivo permeation, and skin retention. Hysteresis loop in the rheogram suggested thixotropy of PDG. Syneresis for gels from day 0-30 days was found to be between 0% and 12.46% w/w. SPF of optimized PDG was 27±0.5. Optimized PDG showed no signs of erythema and edema on Wistar rats. PMMs thus effectively enhanced antioxidant and skin protective effect of curcumin and quercetin.

Development and performance evaluation of self-assembled pH-responsive curcumin-bacterial exopolysaccharide micellar conjugates as bioactive delivery system.

The present study reports the synthesis of micellar conjugates, wherein curcumin (Cur), a bioactive compound with poor bioavailability, was covalently bonded to a bacterial exopolysaccharide (EPS). These conjugates were synthesized by utilizing succinic acid that linked Cur to the pyranosyl moiety of the EPS. The Cur-EPS conjugates appeared as spherical micelles in aqueous solution and were found to have an average hydrodynamic diameter of 254 ± 2.7 nm. The micellar conjugates showed superior stability than Cur as evident from their negative surface charge (-27 ± 1.8 mV) and low polydispersity index (PDI) (0.33 ± 0.04). The in vitro studies on release kinetics helped elucidate the pH-responsive characteristics of the Cur-EPS conjugate, as 87.50 ± 1.45 % of Cur was released at an acidic pH of 5.6, in contrast to 30.15 ± 2.61 % at systemic pH of 7.4 at 150 h. The conjugates were hemocompatible and exhibited cytotoxic effect against the osteosarcoma cell line (MG-63) after 48 h treatment. They also demonstrated superior antibacterial, antibiofilm, and antioxidant activities in comparison to free Cur. Therefore, the Cur-EPS conjugates have potential pharmaceutical applications as therapeutic biomaterial that can be applied as a drug delivery system.

Conception of pH-sensitive calcium alginate/poly vinyl alcohol hydrogel beads for controlled oral curcumin delivery systems. Antibacterial and antioxidant properties.

Curcumin, a bioactive compound derived from the rhizome of Curcuma longa, has gained widespread attention for its potential therapeutic properties, including anti-inflammatory, antioxidant and anticancer effects. However, its poor aqueous solubility, instability and limited bioavailability have hindered its clinical applications. New beads formulations based on sodium alginate biopolymer (SA) and poly vinyl alcohol (PVA) were successfully prepared and evaluated as a potential drug vehicle for extended release of curcumin (Cur). Pristine and curcumin loaded calcium alginate/poly vinyl alcohol beads (CA/PVA and CA/PVA/Cur) at different compositions of SA and PVA were prepared by an ionotropic gelation method of SA followed by two freeze-thawing (FT) cycles for further crosslinking of PVA. Characterization techniques, such as scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), UV-Visible spectroscopy, thermogravimetric analysis (TGA) and x-ray diffraction (XRD) were used to confirm the successful microencapsulation of curcumin within the CA/PVA microcapsules. Furthermore, the swelling of pristine beads, pH-sensitive properties and in vitro release studies of curcumin loaded beads were investigated at 37 °C in simulated gastric fluid (SGF), simulated intestinal fluid (SIF) and simulated colonic fluid (SCF). The effect of the polymer blend ratio, the encapsulation efficiency (EE %) of curcumin, the loading capacity (LC µg/mg), the sphericity factor (SF), the antioxidant activity of the elaborated beads and their antimicrobial properties against bacteria and fungi were just as much evaluated. The obtained results indicate that the swelling and the behavior of the developed beads were influenced by the pH of the test medium and the PVA content. The introduction of PVA into the SA matrix greatly enhanced the physicochemical properties, the encapsulation efficiency and the loading capacity of the elaborated microparticles. Results also suggested that the antioxidant activity of the loaded beads (CA/PVA/Cur) showed a higher DPPH radical scavenging activity while the bacterial and fungal strains proved sensitive to the different formulations used in the assay. Moreover, the important drug encapsulation efficiency and the sustainable drug release of these materials make them promising for the development of new drug carrier systems for colon targeting.

Exploring the emulsification potential of chitosan modified with phenolic acids: Emulsifying properties, functional activities, and application in curcumin encapsulation.

This study successfully grafted caffeic acid and 3,4-dihydroxybenzoic acid into chitosan through a coupling reaction, yielding grafting ratio of 8.93 % for caffeic acid grafted chitosan (CA-GC) and 9.15 % for 3,4-dihydroxybenzoic acid grafted chitosan (DHB-GC) at an optimal concentration of 4 mmol phenolic acids. The characterization of modified chitosans through ultraviolet visible spectrometer (UV-vis), Fourier transform infrared spectrometer (FTIR), proton nuclear magnetic resonance (1H NMR), and x-ray photoelectron spectrometer (XPS) confirmed the successful grafting of phenolic acids. In the subsequent step of emulsion preparation, confocal laser scanning microscope images confirmed the formation of O/W (oil-in-water) emulsions. The phenolic acid-grafted chitosans exhibited better emulsification properties compared to native chitosan, such as reduced droplet size, more uniform emulsion droplet distribution, increased ζ-potential, and enhanced emulsifying activity and stability. Moreover, the modified chitosans demonstrated increased antioxidant activities (evidenced by DPPH and ß-carotene assays) and displayed greater antimicrobial effects against E. coli and S. aureus. Its efficacy in curcumin encapsulation was also notable, with improved encapsulation efficiency, sustained release rates, and enhanced storage and photostability. These findings hint at the potential of modified chitosans as an effective emulsifier.

Development of sorghum arabinoxylan-soy protein isolate composite nanoparticles for delivery of curcumin: Effect of polysaccharide content on stability and in vitro digestibility.

The purpose of this study was to fabricate composite nanoparticles using soy protein isolate (SPI) and sorghum bran arabinoxylan (AX) for the delivery of curcumin (Cur). The influences of AX concentrations on the physicochemical characteristic, stability and bioaccessibility of curcumin were investigated. The findings showed that the encapsulation efficiency of curcumin obviously increased upon incorporating AX in comparison to SPI-Cur particles. Hydrogen bonds and hydrophobic interactions were the primary driving forces for the formation of SPI-Cur-AX nanoparticles (SCA). SCA nanoparticles with 1.00 % AX exhibited a uniform size with orderly distribution, suggesting its remarkable physical stability due to the strengthened electrostatic repulsion. However, excessive AX led to aggregation of particles, a noticeable increase in size, and subsequently, a reduction in stability. Due to the heightened free radical scavenging capacity of sorghum AX, SCA nanoparticles exhibited superior antioxidant capabilities. Compared to free curcumin, encapsulation within composite particles significantly enhanced the retention rate and bioaccessibility of curcumin. This improvement was attributed to the potent emulsification ability of AX, which coordinated with bile salt to promote the transfer of curcumin into micelles. The research provides an effective strategy for developing food-grade delivery carriers aimed at enhancing dispersibility, stability and bioaccessibility of the fat-soluble bioactives.

Carboxymethyl chitosan-N-alkylimine derivatives: Synthesis, characterization and use for preservation of symbiotic biofertilizer bacteria on chickpea seeds.

A series of carboxymethyl chitosan-N-alkylimine derivatives with side chain length of 4 to 10 carbons (CMCS-n, n = 4, 6, 8, 10) was prepared in a one-step solvent-free synthesis using Schiff base chemistry. The modified polysaccharides were characterized by their spectral, thermal and physical properties. The prepared polymers demonstrated an ability to spontaneous self-assembly with a clear correlation between critical aggregation concentration and the chain length of the alkyl substituent. N-alkylimine-CMCS derivatives were found to deliver hydrophobic (curcumin) and hydrophilic (ascorbic acid) active agents in unfavorable environments of water and oil, respectively. Then, N-alkylimine-CMCS derivatives were used as a platform for the delivery of symbiotic gram-positive bacteria Bacillus subtilis CJ onto chickpea seeds. These bacteria demonstrated a significantly higher survival rate (106 CFU/mL) in dried CMCS-6 derivative film than in other films tested. The seeds treated with N-alkylimine-CMCS coatings that contained B. subtilis CJ demonstrated up to 100-fold increase of this bacterial population on the seedlings in comparison to the pristine CMCS.

Study of the self-assembly, drug encapsulating and delivering characteristics of short chain amylose-based type 3 resistant starch nanoparticles from Canna edulis.

In developing type 3 resistant starch (RS3) from Canna edulis for use as functional food ingredients, we investigated the synthesis of C. edulis RS3 nanoparticles. Simultaneously, we explored the potential of C. edulis short-chain amylose (SCA)-based RS3 nanoparticles (RS3N) as a targeted delivery system, with a specific focus on colon targeting, yielding promising insights. Our study revealed that the degree of polymerization (DP) of C. edulis SCA, particularly the chains of DP 36- 100, exhibited a robust correlation with the particle size and physicochemical characteristics of C. edulis SCA-based RS3N. Additionally, recrystallization temperature variation (4, 25, and 45 °C) significantly influenced the self-assembly behavior of C. edulis SCA, with the preparation at 4 °C resulting in more uniform particle size distributions. In further expanding the scope of applications for C. edulis SCA-based RS3N, we harnessed the potential of Fe3O4 and curcumin (CUR) as guest molecules to assess drug encapsulation and colon-targeting capabilities. Incorporating Fe3O4 into the self-assembly system led to the production of magnetic RS3N, confirming the successful encapsulation of Fe3O4 within C. edulis SCA-based RS3N. Furthermore, in vitro experiments have demonstrated that CUR-RS3N was stable in the gastrointestinal tract and gradually released curcumin with fermentation in the colonic environment. Collectively, these findings provide invaluable insights into the intricate self-assembly behavior of C. edulis SCA with varying fine structures and recrystallization temperatures during RS3N formation. Moreover, they underscore the colon-targeted properties of C. edulis SCA-based RS3N, opening promising avenues for its application within the food industry, particularly in advanced controlled drug delivery systems.

Design, synthesis, and evaluation of cyclic C7-bridged monocarbonyl curcumin analogs containing an o-methoxy phenyl group as potential agents against gastric cancer.

The structure-activity relationship (SAR) between toxicity and the types of linking ketones of C7 bridged monocarbonyl curcumin analogs (MCAs) was not clear yet. In the pursuit of effective and less cytotoxic chemotherapeutics, we conducted a SAR analysis using various diketene skeletons of C7-bridged MCAs, synthesized cyclic C7-bridged MCAs containing the identified low-toxicity cyclopentanone scaffold and an o-methoxy phenyl group, and assessed their anti-gastric cancer activity and safety profile. Most compounds exhibited potent cytotoxic activities against gastric cancer cells. We developed a quantitative structure-activity relationship model (R2 > 0.82) by random Forest method, providing important information for optimizing structure. An optimized compound 2 exhibited in vitro and in vivo anti-gastric cancer activity partly through inhibiting the AKT and STAT3 pathways, and displayed a favorable in vivo safety profile. In summary, this paper provided a promising class of MCAs and a potential compound for the development of chemotherapeutic drugs.