Development of High-Energy Amorphous Solid Dispersion of Nanosized Nobiletin, a Citrus Polymethoxylated Flavone, with Improved Oral Bioavailability

Onoue, Satomi; Uchida, Atsushi; Takahashi, H.; Seto, Yoshiki; Kawabata, Youhei; Ogawa, Kazunori; Yuminoki, Kayo; Hashimoto, Naofumi; Yamada, Shizuo

doi:10.1002/jps.22585

Cited by 66 publications

(46 citation statements)

References 25 publications

(29 reference statements)

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“…In other phytochemicals, it is known that the solubility, oral absorption, antiinflammation activity, and neuroprotective effects (in terms of reversing AlCl 3 -induced neuronal damage, biochemical alterations, and memory impairment in mice) of curcumin have been dramatically enhanced by the preparation of curcumin nanoformulations [48]. In citrus flavonoids, high-energy amorphous solid dispersion of nanosized nobiletin with improved oral bioavailability (13-fold) and brain distribution (sevenfold) compared to those of crystalline nobiletin has been developed [49]. However, studies of safe toxicological profiles of flavonoid nanoformulations and their efficacy in in vitro and in vivo models and human trials need to be conducted to establish their effectiveness in clinical applications as improved therapeutic agents for dementia treatment.…”

Section: Practical Issues Of Citrus Flavonoids As Pharmacological Agentsmentioning

confidence: 99%

Citrus Flavonoids and Effects in Dementia and Age-Related Cognitive Decline

Hwang

Shih

Yen

2015

Diet and Nutrition in Dementia and Cognitive Decline

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Section: Practical Issues Of Citrus Flavonoids As Pharmacological Agentsmentioning

confidence: 99%

Citrus Flavonoids and Effects in Dementia and Age-Related Cognitive Decline

Hwang

Shih

Yen

2015

Diet and Nutrition in Dementia and Cognitive Decline

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“…The higher solubility is due to the lack of the crystal structure and the rapid dissolution of the supporting matrix. Quercetin, 196 silymarin, 197 and nobiletin 198 were recently formulated as solid dispersions. Onoue and colleagues showed that wetmilled nobiletin nanoparticles showed 13-fold higher bioavailability than the crystalline form.…”

Section: Amorphous Solid Dispersionmentioning

confidence: 99%

Flavonoids as dietary regulators of nuclear receptor activity

et al. 2013

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Metabolic diseases such as obesity, type II diabetes, and dyslipidemia are a rising cause of mortality worldwide. The progression of many metabolic diseases is fundamentally regulated on the transcriptional level by a family of ligand-activated transcription factors, called nuclear receptors, which detect and respond to metabolic changes. Their role in maintaining metabolic homeostasis makes nuclear receptors an important pharmaceutical and dietary target. This review will present the growing evidence that flavonoids, natural secondary plant metabolites, are important regulators of nuclear receptor activity. Structural similarities between flavonoids and cholesterol derivatives combined with the promiscuous nature of most nuclear receptors provide a wealth of possibilities for pharmaceutical and dietary modulation of metabolism. While the challenges of bringing flavonoid-derived therapeutics to the market are significant, we consider this rapidly growing field to be an essential aspect of the functional food initiative and an important mine for pharmaceutical compounds.

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“…Therefore, a citrus processing waste can be potentially converted into a valuable functional ingredient. However, NOB exhibits poor water solubility because all hydroxyl groups in the structure are methoxylated, leading to low oral bioavailability, thus limiting the practical uses of NOB [6].…”

Section: Introductionmentioning

confidence: 99%

Preparation and Characterisation of Nobiletin-Loaded Nanostructured Lipid Carriers

Huang

Dou

et al. 2017

Journal of Nanomaterials

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The objective of this manuscript was to investigate and optimise the potential of nanostructured lipid carriers (NLCs) as a carrier system for nobiletin (NOB), which was prepared by high-pressure homogenisation method. Additionally, this study was focused on the application of NOB-loaded NLC (NOB-NLC) in functional food. Response surface method with a three-level Box-Behnken design was validated through analysis of variance, and the robustness of the design was confirmed through the correspondence between the values measured in the experiments and the predicted ones. Properties of the prepared NOB-NLC, such asaverage, polydispersity, entrapment efficiency, zeta potential, morphology, and crystallinity, were investigated. NOB-NLC exhibited a spherical shape with a diameter of 112.27 ± 5.33 nm, zeta potential of −35.1 ± 2.94 mV, a polydispersity index of 0.251 ± 0.058, and an EE of 81.06% ± 6.02%. Results from X-ray diffraction and differential scanning calorimetry of NOB-NLC reviewed that the NOB crystal might be converted to an amorphous state. Fourier transform infrared spectroscopic analysis demonstrated that chemical interaction was absent between the compound and lipid mixture in NOB-NLC.

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Development of High-Energy Amorphous Solid Dispersion of Nanosized Nobiletin, a Citrus Polymethoxylated Flavone, with Improved Oral Bioavailability

Cited by 66 publications

References 25 publications

Citrus Flavonoids and Effects in Dementia and Age-Related Cognitive Decline

Citrus Flavonoids and Effects in Dementia and Age-Related Cognitive Decline

Flavonoids as dietary regulators of nuclear receptor activity

Preparation and Characterisation of Nobiletin-Loaded Nanostructured Lipid Carriers

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