Enhanced oral bioavailability of naringenin administered in a mixed micelle formulation with Pluronic F127 and Tween 80 in rats

Song, Im‐Sook; Cha, Jin-Sun; Choi, Min‐Koo

doi:10.1007/s40005-015-0216-x

Cited by 14 publications

(5 citation statements)

References 22 publications

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“…The delivery of NRG via micelles has been studied by several research groups. In 2015, the impact of encapsulating NRG in a mixed micelle formation of Pluronic F127 and Tween 80 on its oral bioavailability was evaluated in male SD rats [ 98 ]. Pluronic F127 (Poloxamer 407) is a non-ionic surfactant, and its micellar properties are highly soluble and suitable for drug delivery [ 99 ].…”

Section: Nrg Nano-scaled Delivery Systemsmentioning

confidence: 99%

“…The in vivo investigation of their pharmacokinetic parameters showed a significant enhancement in NRG solubility (by 27-fold), its bioavailability (up to 26.9% following oral administration), and intestinal permeability (1.7-fold) compared to free NRG administration. Hence, it could be concluded that NRG-loaded micelles are more effective than oral administration of free NRG [ 98 ].…”

Section: Nrg Nano-scaled Delivery Systemsmentioning

confidence: 99%

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Naringenin Nano-Delivery Systems and Their Therapeutic Applications

et al. 2021

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Naringenin (NRG) is a polyphenolic phytochemical belonging to the class of flavanones and is widely distributed in citrus fruits and some other fruits such as bergamot, tomatoes, cocoa, and cherries. NRG presents several interesting pharmacological properties, such as anti-cancer, anti-oxidant, and anti-inflammatory activities. However, the therapeutic potential of NRG is hampered due to its hydrophobic nature, which leads to poor bioavailability. Here, we review a wide range of nanocarriers that have been used as delivery systems for NRG, including polymeric nanoparticles, micelles, liposomes, solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), nanosuspensions, and nanoemulsions. These nanomedicine formulations of NRG have been applied as a potential treatment for several diseases, using a wide range of in vitro, ex vivo, and in vivo models and different routes of administration. From this review, it can be concluded that NRG is a potential therapeutic option for the treatment of various diseases such as cancer, neurological disorders, liver diseases, ocular disorders, inflammatory diseases, skin diseases, and diabetes when formulated in the appropriate nanocarriers.

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Section: Nrg Nano-scaled Delivery Systemsmentioning

confidence: 99%

Section: Nrg Nano-scaled Delivery Systemsmentioning

confidence: 99%

Naringenin Nano-Delivery Systems and Their Therapeutic Applications

et al. 2021

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“…Various pharmaceutical strategies, such as formulating with solubility enhancers, P-gp inhibitor, and metabolic inhibitors have been undertaken to improve the pharmacokinetic and biopharmaceutical properties of naringenin in achieving the clinical relevance [118]. However, nanotechnology-based formulation designing has emerged as a prospective strategy over others to eliminate pharmaceutical incompetencies and to achieve better therapeutic efficacy of naringenin.…”

Section: Naringeninmentioning

confidence: 99%

Plant-Based Antidiabetic Nanoformulations: The Emerging Paradigm for Effective Therapy

Dewanjee

Chakraborty

Mukherjee

et al. 2020

IJMS

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Diabetes mellitus is a life-threatening metabolic syndrome. Over the past few decades, the incidence of diabetes has climbed exponentially. Several therapeutic approaches have been undertaken, but the occurrence and risk still remain unabated. Several plant-derived small molecules have been proposed to be effective against diabetes and associated vascular complications via acting on several therapeutic targets. In addition, the biocompatibility of these phytochemicals increasingly enhances the interest of exploiting them as therapeutic negotiators. However, poor pharmacokinetic and biopharmaceutical attributes of these phytochemicals largely restrict their clinical usefulness as therapeutic agents. Several pharmaceutical attempts have been undertaken to enhance their compliance and therapeutic efficacy. In this regard, the application of nanotechnology has been proven to be the best approach to improve the compliance and clinical efficacy by overturning the pharmacokinetic and biopharmaceutical obstacles associated with the plant-derived antidiabetic agents. This review gives a comprehensive and up-to-date overview of the nanoformulations of phytochemicals in the management of diabetes and associated complications. The effects of nanosizing on pharmacokinetic, biopharmaceutical and therapeutic profiles of plant-derived small molecules, such as curcumin, resveratrol, naringenin, quercetin, apigenin, baicalin, luteolin, rosmarinic acid, berberine, gymnemic acid, emodin, scutellarin, catechins, thymoquinone, ferulic acid, stevioside, and others have been discussed comprehensively in this review.

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“…Amorphous ternary solid dispersions of NAR, Poloxamer 188, and Neusilin US2, prepared by hot-melt extrusion, enabled an increase in the release of NAR within 2 h from 22% to 77% [ 20 ]. The NAR-loaded mixed micelle formulation with NAR:Pluronic F127:Tween 80 in a weight ratio of 1:10:0.2, prepared by a thin-film hydration method, increased the NAR solubility 27-fold and also improved the bioavailability in rats from 4.1 to 26.9% [ 21 ].…”

Section: Introductionmentioning

confidence: 99%

The Systems of Naringenin with Solubilizers Expand Its Capability to Prevent Neurodegenerative Diseases

Stasiłowicz-Krzemień

Gołębiewski

Płazińska

et al. 2022

IJMS

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Background: Naringenin (NAR) is a flavonoid with excellent antioxidant and neuroprotective potential that is limited by its low solubility. Thus, solid dispersions with β-cyclodextrin (β-CD), hydroxypropyl-β-cyclodextrin (HP-β-CD), hydroxypropylmethylcellulose (HPMC), and microenvironmental pH modifiers were prepared. Methods: The systems formation analysis was performed by X-Ray Powder Diffraction (XRPD) and Fourier-transform infrared spectroscopy (FT-IR). Water solubility and dissolution rates were studied with a pH of 1.2 and 6.8. In vitro permeability through the gastrointestinal tract (GIT) and the blood-brain barrier (BBB) was assessed with the parallel artificial membrane permeability assay (PAMPA) assay. The antioxidant activity was studied with the 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and cupric ion reducing antioxidant capacity (CUPRAC) assays, while in vitro enzymes studies involved the inhibition of acetylcholinesterase, butyrylcholinesterase, and tyrosinase. For the most promising system, in silico studies were conducted. Results: NAR solubility was increased 458-fold by the solid dispersion NAR:HP-β-CD:NaHCO3 in a mass ratio of 1:3:1. The dissolution rate was elevated from 8.216% to 88.712% in a pH of 1.2 and from 11.644% to 88.843% in a pH of 6.8 (within 3 h). NAR GIT permeability, described as the apparent permeability coefficient, was increased from 2.789 × 10−6 cm s−1 to 2.909 × 10−5 cm s−1 in an acidic pH and from 1.197 × 10−6 cm s−1 to 2.145 × 10−5 cm s−1 in a basic pH. NAR BBB permeability was established as 4.275 × 10−6 cm s−1. The antioxidant activity and enzyme inhibition were also increased. Computational studies confirmed NAR:HP-β-CD inclusion complex formation. Conclusions: A significant improvement in NAR solubility was associated with an increase in its biological activity.

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Enhanced oral bioavailability of naringenin administered in a mixed micelle formulation with Pluronic F127 and Tween 80 in rats

Cited by 14 publications

References 22 publications

Naringenin Nano-Delivery Systems and Their Therapeutic Applications

Naringenin Nano-Delivery Systems and Their Therapeutic Applications

Plant-Based Antidiabetic Nanoformulations: The Emerging Paradigm for Effective Therapy

The Systems of Naringenin with Solubilizers Expand Its Capability to Prevent Neurodegenerative Diseases

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