Enhanced bioactivity and efficient delivery of quercetin through nanoliposomal encapsulation using rice bran phospholipids.

Quercetin is a phenolic compound occurring in many food plants and agricultural crops. It is reported to possess various health-promoting properties. However, the poor bioavailability of quercetin, due to its low aqueous solubility and its degradation during digestion, limits its nutraceutical applications. This study aimed to encapsulate quercetin in nanoliposomes using rice-bran phospholipids for its efficient delivery and controlled release, the protection of its structural stability, and enhancement of its bioactivity. Nanoliposomal encapsulation of quercetin by thin film-sonication method yielded spherical nanoparticles (157.33 ± 23.78 nm) with high encapsulation efficiency (84.92 ± 0.78%). Storage stability studies showed that nanoliposomal quercetin was stable at 4 °C and 27 °C for 6 and 5 months, respectively, as indicated by unchanged antioxidant activity and quercetin retention. Nanoliposomal quercetin showed a slow, limited release pattern in simulated gastric fluid (SGF), and an initial burst release followed by a slow constant releasing pattern in simulated intestinal fluid (SIF). A 1004-fold increase in 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging activity was observed in quercetin nanoliposomes (SC50 = 4.04 ± 0.01 ppm) compared to non-encapsulated quercetin (SC50 = 4053.03 ± 5.61 ppm). Similarly, the anti-angiogenic activity of quercetin, as evaluated by duck embryo chorioallantoic membrane (CAM) assay, was enhanced twofold to fivefold by nanoliposomal encapsulation. This study showed that nanoliposomal encapsulation in rice-bran phospholipids enhanced the radical-scavenging and anti-angiogenic activities of quercetin. Furthermore, this study demonstrated that nanoliposomes can serve as efficient oral delivery system for quercetin. © 2018 Society of Chemical Industry.

Rodriguez EB ，Almeda RA ，Vidallon MLP ，Reyes CT ... -  《-》

Encapsulation of Lipophilic Polyphenols into Nanoliposomes Using pH-Driven Method: Advantages and Disadvantages.

Peng S ，Zou L ，Zhou W ，Liu W ，Liu C ，McClements DJ ... -  《-》

Bovine serum albumin nanoparticle promotes the stability of quercetin in simulated intestinal fluid.

Fang R ，Hao R ，Wu X ，Li Q ，Leng X ，Jing H ... -  《-》

Enhancement of solubility, antioxidant ability and bioavailability of taxifolin nanoparticles by liquid antisolvent precipitation technique.

Taxifolin is a kind of flavanonol, whose antioxidant ability is superior to that of ordinary flavonoids compounds owing to its special structure. However, its low bioavailability is a major obstacle for biomedical applications, so the experiment is designed to prepare taxifolin nanoparticles by liquid antisolvent precipitation (LAP) to improve its bioavailability. We selected ethanol as solvent, deionized water as antisolvent, and investigated primarily the type of surfactant and adding amount, drug concentration, volume ratio of antisolvent to solvent, precipitation temperature, dropping speed, stirring speed, stirring time factors affecting drug particles size. Results showed that the poloxamer 188 was selected as the surfactant and the particle size of taxifolin obviously reduced with the increase of the poloxamer 188 concentration, the drug concentration and the dropping speed from 0.08% to 0.45%, from 0.04 g/ml to 0.12 g/ml, from 1 ml/min to 5 ml/min, respectively, when the volume ratio of antisolvent to solvent increased from 2.5 to 20, the particle size of taxifolin first increased and then decreased, the influence of precipitation temperature, stirring speed, stirring time on particle size were not obvious, but along with the increase of mixing time, the drug solution would separate out crystallization. The optimum conditions were: the poloxamer 188 concentration was 0.25%, the drug concentration was 0.08 g/ml, the volume ratio of antisolvent to solvent was 10, the precipitation temperature was 25 °C, the dropping speed was 4 ml/min, the stirring speed was 800 r/min, the stirring time was 5 min. Taxifolin nanosuspension with a MPS of 24.6 nm was obtained under the optimum conditions. For getting taxifolin nanoparticles, the lyophilization method was chosen and correspondingly γ-cyclodextrin was selected as cryoprotectant from γ-cyclodextrin, mannitol, lactose, glucose. Then the properties of raw taxifolin and taxifolin nanoparticles were characterized by scanning electron microscopy (SEM), fourier-transform infrared spectroscopy (FTIR), high performance liquid chromatography-mass spectrometry (LC-MS), X-ray diffraction (XRD), differential scanning calorimetry (DSC), and thermo gravimetric (TG), and the conclusion was drawn that taxifolin nanoparticles can be converted into an amorphous form but its chemical construction cannot been changed. Furthermore, dissolving capability test, 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging activity and reducing power assay, solvent residue test were also carried out. The experimental data showed that the solubility and the dissolution rate of taxifolin nanoparticles were about 1.72 times and 3 times of raw taxifolin, the bioavailability of taxifolin nanoparticles increased 7 times compared with raw taxifolin, and the antioxidant capacity of taxifolin nanoparticles was also superior to raw taxifolin. Furthermore, the residual ethanol of the taxifolin nanoparticles was less than the ICH limit for class 3 solvents of 5000 ppm or 0.5% for solvents and could be used for pharmaceutical. These results suggested that taxifolin nanoparticles might have potential value to become a new oral taxifolin formulation with high bioavailability.

Zu Y ，Wu W ，Zhao X ，Li Y ，Wang W ，Zhong C ，Zhang Y ，Zhao X ... -  《-》

Nanoencapsulation in low-molecular-weight chitosan improves in vivo antioxidant potential of black carrot anthocyanin.

Anthocyanins are flavonoids that are potential antioxidant, anti-inflammatory, anti-obesity, and anti-carcinogenic nutraceutical ingredients. However, low chemical stability and low bioavailability limit the use of anthocyanins in food. Nanoencapsulation using biopolymers is a recent successful strategy for stabilization of anthocyanins. This study reports the development, characterization, and antioxidant activity of black carrot anthocyanin-loaded chitosan nanoparticles (ACNPs). The ionic gelation technique yielded the ACNPs. The mean hydrodynamic diameter d and polydispersity index PDI of chitosan nanoparticles and ACNPs were found to be d = 455 nm and PDI = 0.542 respectively for chitosan nanoparticles and d = 274 nm and PDI = 0.376 respectively for ACNPs. The size distribution was bimodal. The surface topography revealed that the ACNPs are spherical and display a coacervate structure. Fourier transform infrared analysis revealed physicochemical interactions of anthocyanins with chitosan. The loading process could achieve an encapsulation efficiency of 70%. The flow behavior index η of encapsulated ACNPs samples revealed Newtonian and shear thickening characteristics. There was a marginal reduction in the in vitro antioxidant potential of anthocyanins after nanoencapsulation, as evidenced from 2,2-diphenyl-1-picrylhydrazyl, ferric reducing antioxidant power, and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) assays. Interestingly, the in vivo antioxidant potential of anthocyanins improved following nanoencapsulation, as observed in the serum antioxidant assays. The optimized nanoencapsulation process resulted in spherical nanoparticles with appreciable encapsulation efficiency. The nanoencapsulation process improved the in vivo antioxidant activity of anthocyanins, indicating enhanced stability and bioavailability. The promising antioxidant activity of the ACNPs suggests a potential for utilization as a nutraceutical supplement. © 2021 Society of Chemical Industry.

Chatterjee NS ，Dara PK ，Perumcherry Raman S ，Vijayan DK ，Sadasivam J ，Mathew S ，Ravishankar CN ，Anandan R ... -  《-》