Nanospray Drying as a Novel Tool to Improve Technological Properties of Soy Isoflavone Extracts

Gaudio, Pasquale Del; Sansone, Francesca; Mencherini, Teresa; Cicco, Felicetta De; Russo, Paola; Aquino, Rita Patrizia

doi:10.1055/s-0042-110179

Cited by 16 publications

(11 citation statements)

References 29 publications

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“…The morphology and dimensions of the microsystems were assessed as reported by Del Gaudio et al [44]. Briefly, using SEM, the microparticles were coated with Au/Pd and then observed using a scanning electron microscope (Scanning Microscope JSM 6400, Jeol Ltd.) at different extensions.…”

Section: Morphology and Particle Size Evaluationmentioning

confidence: 99%

Halimium halimifolium: From the Chemical and Functional Characterization to a Nutraceutical Ingredient Design

et al. 2019

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Halimium halimifolium (Hh) is a shrub used in Algerian folk medicine to treat gastrointestinal pain. An UHPLC-PDA-ESI/MSn method was developed to identify the metabolic profile of the traditionally used infusion (Hh-A) from the aerial parts. The structures of flavanols were confirmed by NMR analysis after the isolation procedure from a hydrohalcolic extract (Hh-B) that also allowed for the identification of phenolic acids, an aryl butanol glucoside, and different derivatives of quercetin, myricetin, and kaempferol. Tiliroside isomers were the chemical markers of Hh-A and Hh-B (54.33 and 36.00 mg/g, respectively). Hh-A showed a significant scavenging activity both against the radicals 1,1-diphenyl-2-picrylhydrazyl and 2,2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (EC50 = 10.49 µg/mL and TEAC value = 1.98 mM Trolox/mg infusion) and the lipopolysaccharide-induced reactive oxygen species release in A375 and HeLa cells. Moreover, the antihyperglycemic properties, by inhibiting the α-amylase and α-glucosidase enzymes (IC50 = 0.82 mg/mL and 25.01 µg/mL, respectively), were demonstrated. To upgrade the therapeutic effect, a microencapsulation process is proposed as a strategy to optimize stability, handling, and delivery of bioactive components, avoiding the degradation and loss of the biological efficacy after oral intake. Hh-loaded microparticles were designed using cellulose acetate phthalate as the enteric coating material and spray drying as a production process. The results showed a satisfactory process yield (67.9%), encapsulation efficiency (96.7%), and micrometric characteristics of microparticles (laser-scattering, fluorescent, and scanning electron microscopy). In vitro dissolution studies (USPII-pH change method) showed that Hh-loaded microparticles are able to prevent the release and degradation of the bioactive components in the gastric tract, releasing them into the intestinal environment.

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Section: Morphology and Particle Size Evaluationmentioning

confidence: 99%

Halimium halimifolium: From the Chemical and Functional Characterization to a Nutraceutical Ingredient Design

et al. 2019

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“…Genistein is widely studied as a phytoestrogen which protects against ischemic strokeinduced brain injury. However, the bioavailability of genistein is limited because of its poor water and lipid solubility [31]. Genistein-3'-sodium sulfonate (GSS) is a sulfonated product of genistein, which has a better water solubility than genistein.…”

Section: Ivyspringmentioning

confidence: 99%

Genistein-3′-sodium sulfonate Attenuates Neuroinflammation in Stroke Rats by Down-Regulating Microglial M1 Polarization through α7nAChR-NF-κB Signaling Pathway

Liu¹,

Liu²,

Xiong³

et al. 2021

Int. J. Biol. Sci.

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Microglial M1 depolarization mediated prolonged inflammation contributing to brain injury in ischemic stroke. Our previous study revealed that Genistein-3′-sodium sulfonate (GSS) exerted neuroprotective effects in ischemic stroke. This study aimed to explore whether GSS protected against brain injury in ischemic stroke by regulating microglial M1 depolarization and its underlying mechanisms. We established transient middle cerebral artery occlusion and reperfusion (tMCAO) model in rats and used lipopolysaccharide (LPS)-stimulated BV2 microglial cells as in vitro model. Our results showed that GSS treatment significantly reduced the brain infarcted volume and improved the neurological function in tMCAO rats. Meanwhile, GSS treatment also dramatically reduced microglia M1 depolarization and IL-1β level, reversed α7nAChR expression, and inhibited the activation of NF-κB signaling in the ischemic penumbra brain regions. These effects of GSS were further verified in LPS-induced M1 depolarization of BV2 cells. Furthermore, pretreatment of α7nAChR inhibitor (α-BTX) significantly restrained the neuroprotective effect of GSS treatment in tMCAO rats. α-BTX also blunted the regulating effects of GSS on neuroinflammation, M1 depolarization and NF-κB signaling activation. This study demonstrates that GSS protects against brain injury in ischemic stroke by reducing microglia M1 depolarization to suppress neuroinflammation in peri-infarcted brain regions through upregulating α7nAChR and thereby inhibition of NF-κB signaling. Our findings uncover a potential molecular mechanism for GSS treatment in ischemic stroke.

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“…However, besides being challenging to synthesize, these derivatives are still not soluble enough and/or show poorer biological activity than unmodified DAI. The second approach is to encapsulate DAI and related compounds in polymeric nanoparticles composed of, for example, hypromellose [36], carboxymethyl cellulose [37], zein [38], Eudragit E100-polyvinyl alcohol [39], poly(D,L)lactic acid [40], polymeric dendrimers [41,42], and polymeric microparticles composed of gelatin [43] or chitosan [44]. The third common approach is inclusion complexation of DAI with different cyclodextrins (CDs) and their derivatives, which was found to significantly improve its bioavailability, cellular membrane penetration, and therapeutic properties [45][46][47][48].…”

Section: Introductionmentioning

confidence: 99%

Improved Pharmacokinetics and Tissue Uptake of Complexed Daidzein in Rats

et al. 2020

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The pharmacokinetic profile and tissue uptake of daidzein (DAI) was determined in rat serum and tissues (lungs, eyes, brain, heart, spleen, fat, liver, kidney, and testes) after intravenous and intraperitoneal administration of DAI in suspension or complexed with ethylenediamine-modified γ-cyclodextrin (GCD-EDA/DAI). The absolute and relative bioavailability of DAI suspended (20 mg/kg i.v. vs. 50 mg/kg i.p.) and complexed (0.54 mg/kg i.v. vs. 1.35 mg/kg i.p.) was determined. After i.p. administration, absorption of DAI complexed with GCD-EDA was more rapid (tmax = 15 min) than that of DAI in suspension (tmax = 45 min) with a ca. 3.6 times higher maximum concentration (Cmax = 615 vs. 173 ng/mL). The i.v. half-life of DAI was longer in GCD-EDA/DAI complex compared with DAI in suspension (t0.5 = 380 min vs. 230 min). The volume of distribution of DAI given i.v. in GCD-EDA/DAI complex was ca. 6 times larger than DAI in suspension (38.6 L/kg vs. 6.2 L/kg). Our data support the concept that the pharmacokinetics of DAI suspended in high doses are nonlinear. Increasing the intravenous dose 34 times resulted in a 5-fold increase in AUC. In turn, increasing the intraperitoneal dose 37 times resulted in a ca. 2-fold increase in AUC. The results of this study suggested that GCD-EDA complex may improve DAI bioavailability after i.p. administration. The absolute bioavailability of DAI in GCD-EDA inclusion complex was ca. 3 times greater (F = 82.4% vs. 28.2%), and the relative bioavailability was ca. 21 times higher than that of DAI in suspension, indicating the need to study DAI bioavailability after administration by routes other than intraperitoneal, e.g., orally, subcutaneously, or intramuscularly. The concentration of DAI released from GCD-EDA/DAI inclusion complex to all the rat tissues studied was higher than after administration of DAI in suspension. The concentration of DAI in brain and lungs was found to be almost 90 and 45 times higher, respectively, when administered in complex compared to the suspended DAI. Given the nonlinear relationship between DAI bioavailability and the dose released from the GCD-EDA complex, complexation of DAI may thus offer an effective approach to improve DAI delivery for treatment purposes, for example in mucopolysaccharidosis (MPS), allowing the reduction of ingested DAI doses.

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Nanospray Drying as a Novel Tool to Improve Technological Properties of Soy Isoflavone Extracts

Cited by 16 publications

References 29 publications

Halimium halimifolium: From the Chemical and Functional Characterization to a Nutraceutical Ingredient Design

Halimium halimifolium: From the Chemical and Functional Characterization to a Nutraceutical Ingredient Design

Genistein-3′-sodium sulfonate Attenuates Neuroinflammation in Stroke Rats by Down-Regulating Microglial M1 Polarization through α7nAChR-NF-κB Signaling Pathway

Improved Pharmacokinetics and Tissue Uptake of Complexed Daidzein in Rats

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