Absorption improvement of tranilast by forming highly soluble nano-size composite structures associated with α-glucosyl rutin via spray drying

Sato, Hideyuki; Fujimori, Miki; Suzuki, Haruo; Kadota, Kazunori; Shirakawa, Yoshiyuki; Onoue, Satomi; Tozuka, Yuichi

doi:10.1016/j.ejpb.2015.02.021

Cited by 28 publications

(9 citation statements)

References 32 publications

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“…However, despite various biological activities, poor solubility in aqueous media (approximately 0.125 g/liter at room temperature) has largely limited its usage owing to its poor bioavailability ( 16 ). Recently, various strategies have been developed to improve the solubility and bioavailability of compounds that are poorly soluble in water ( 17 , 18 ), among which salt formation is the most common and most effective method to increase the solubility and dissolution rates of drugs ( 16 , 19 ). In the present study, we processed rutin into sodium salt [hereafter called sodium rutin (NaR)], which is highly water soluble and bioavailable.…”

Section: Introductionmentioning

confidence: 99%

Sodium rutin ameliorates Alzheimer’s disease–like pathology by enhancing microglial amyloid-β clearance

et al. 2019

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The accumulation of aggregated amyloid-β (Aβ) in the brain is the first critical step in the pathogenesis of Alzheimer’s disease (AD), which also includes synaptic impairment, neuroinflammation, neuronal loss, and eventual cognitive defects. Emerging evidence suggests that impairment of Aβ phagocytosis and clearance is a common phenotype in late-onset AD. Rutin (quercetin-3-rutinoside) has long been investigated as a natural flavonoid with different biological functions in some pathological circumstances. Sodium rutin (NaR), could promote Aβ clearance by increasing microglial by increasing the expression levels of phagocytosis-related receptors in microglia. Moreover, NaR promotes a metabolic switch from anaerobic glycolysis to mitochondrial OXPHOS (oxidative phosphorylation), which could provide microglia with sufficient energy (ATP) for Aβ clearance. Thus, NaR administration could attenuate neuroinflammation and enhance mitochondrial OXPHOS and microglia-mediated Aβ clearance, ameliorating synaptic plasticity impairment and eventually reversing spatial learning and memory deficits. Our findings suggest that NaR is a potential therapeutic agent for AD.

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Section: Introductionmentioning

confidence: 99%

Sodium rutin ameliorates Alzheimer’s disease–like pathology by enhancing microglial amyloid-β clearance

et al. 2019

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“…The inlet temperature of a drying chamber was 120°C, the outlet temperature was 68°C, and the spraying air pressure was 0.2 MPa. The spray-dried powder was stored in a desiccator for sufficient drying before use in a test [ 10 , 11 , 19 ]. The combinations of three kinds of flavonoid composite prepared in this experiment are shown in Table 1 .…”

Section: Methodsmentioning

confidence: 99%

Design and evaluation of a novel flavonoid-based radioprotective agent utilizing monoglucosyl rutin

Aizawa

Sunada

Hirakawa³

et al. 2018

Journal of Radiation Research

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In this study, three novel flavonoid composite materials, created by combining an aglycone [quercetin (QUE), hesperetin (HES) or naringenin (NAR)] with monoglucosyl rutin (MGR), were designed to test for improved radioprotectivity compared with that provided by administration of MGR alone. Aglycone in the MGR-composite state was highly soluble in water, compared with aglycone alone dissolved in dimethyl sulfoxide or distilled water. The antioxidant activity of the three flavonoid composites was as high as that of MGR only. Next, the cytotoxicity test after 30 min treatment of an MGR composite showed a clear reduction in cell viability and suggested that a rapid introduction of aglycone into cells had taken place. In addition, QUE/MGR and HES/MGR composites strongly scavenged intracellular reactive oxygen species (ROS) induced by X-ray irradiation as well as MGR alone did. However, in the colony-formation assay using irradiated Chinese hamster ovary (CHO) cells, the HES/MGR composite showed a stronger radioprotective effect than MGR alone did, but the QUE/MGR composite showed no additional protective effect compared with the control. Furthermore, it was revealed that QUE and QUE/MGR composite treatment had the effect of reducing the glutathione (GSH) content in cells, and that QUE showed a stronger inhibition of PARP activity compared that of HES and NAR. Our data demonstrated that when designing a flavonoid composite as a radioprotective agent, it was necessary to select an appropriate aglycone, considering not only its antioxidant ability but also its inhibitory effect on cell recovery or DNA repair after radiation injury.

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“…However, anticancer drugs administration usually results in side effects, including hair loss, nausea, and vomiting, limiting the dosage and frequency of drugs [32,33]. In addition, a variety of drugs, including natural extracts, are restricted for their poor water solubility with low bioavailability [34,35]. Hesperitin is reported to possess anti-cancer ability, such as prostate cancer and esophageal cancer [22,36,37].…”

Section: Discussionmentioning

confidence: 99%

Hesperitin enhances the ability of daunorubicin by co-loading with MPEG-PCL nanoparticles to induce apoptosis in gastric cancer

Zhen¹,

T²,

Tang³

et al. 2017

Oncotarget

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Tumor targeting delivery system has been suggested as an attractive strategy against tumor progression. And combination chemotherapy is essential and effective in preventing gastric cancer. Hesperitin (HE) has been suggested to exhibit anticancer ability through inducing apoptosis in many tumors without obvious toxicity, and it exerts synergistic anti-cancer ability with other drugs. Clinical application of daunorubicin (DA) in treatment of various cancers has been restricted. Targeted delivery of anti-cancer drugs could reduce their off-target effects and promote their efficacy. In our paper, HE and DA co-loaded methoxy poly (ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL) nanoparticles were prepared through an assembly method. The morphology, particle size (about 38 nm), zeta potential, release profile in vitro, cell proliferation and cytotoxicity effects were investigated. The results suggested that HE and DA could be efficiently loaded into MPEG-PCL nanoparticles synchronously, and in vitro study indicated that they could be released from the nanoparticles in an extended period. in vitro, HE/DA/MPEG-PCL exerted an enhanced cytotoxicity and high apoptosis-inducing activities of gastric cancer cells. Importantly, HE/DA/MPEG-PCL exhibited better cancer targeting and accumulation, enhancing the anti-tumor efficacy with little toxicity. Together, HE/DA/MPEG-PCL promoted the drug target on tumor site with preferable anti-tumor effects, which could be a promising therapeutic strategy against human gastric cancer.

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Absorption improvement of tranilast by forming highly soluble nano-size composite structures associated with α-glucosyl rutin via spray drying

Cited by 28 publications

References 32 publications

Sodium rutin ameliorates Alzheimer’s disease–like pathology by enhancing microglial amyloid-β clearance

Sodium rutin ameliorates Alzheimer’s disease–like pathology by enhancing microglial amyloid-β clearance

Design and evaluation of a novel flavonoid-based radioprotective agent utilizing monoglucosyl rutin

Hesperitin enhances the ability of daunorubicin by co-loading with MPEG-PCL nanoparticles to induce apoptosis in gastric cancer

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