Naringenin nanocrystals for improving anti-rheumatoid arthritis activity

Zhang, Guangshuai; Sun, Guangyuan; Guan, Haishan; Li, Mo; Liu, Yanhua; Tian, Baocheng; Zhang, He; Fu, Qiang

doi:10.1016/j.ajps.2021.09.001

Cited by 24 publications

(9 citation statements)

References 37 publications

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“…The outcomes of all these experiments provided newer insight into the treatment of rheumatoid arthritis. 21 Another study describes the formulation and assessment of naringenin nano-suspensions for enhancing bioavailability. This top-down approach undertakes the application of high-energy ball milling methods for the reduction of nanoparticle size to enhance the saturation solubility of naringenin, ultimately improving its bioavailability.…”

Section: Resultsmentioning

confidence: 99%

“…In the recent past, several studies have reported the ball milling of naringenin for the conversion of naringenin into its nanoparticle forms, and these studies have been added in the Discussion Section. − The clinical and therapeutic efficacy of naringenin is restricted due to its lower bioavailability because of the poor solubility. For the enhancement of its solubility, naringenin nanosuspension was prepared by the milling technique.…”

Section: Resultsmentioning

confidence: 99%

“…Finally, in vivo pharmacokinetics and anti-inflammatory potential of nanosized naringenin were also evaluated. The outcomes of all these experiments provided newer insight into the treatment of rheumatoid arthritis . Another study describes the formulation and assessment of naringenin nano-suspensions for enhancing bioavailability.…”

Section: Resultsmentioning

confidence: 99%

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Enhanced Antioxidant Effects of Naringenin Nanoparticles Synthesized using the High-Energy Ball Milling Method

Ahmad¹,

Prakash

Khan

et al. 2022

ACS Omega

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Naringenin, one of the flavonoid components, is majorly found in and obtained from grapefruits and oranges. Naringenin also acts as a potent antioxidant, which possesses hypolipidemic as well as anti-inflammatory potential. Naringenin reduces the expressions of several inflammatory mediators, viz., NF-κB, cycloxygenase-2, and other cytokine mediators. In spite of having various biological effects, the clinical application of naringenin is restricted due to its very poor aqueous solubility. In the present study, the high-energy ball milling method was employed for the preparation of naringenin nanoparticles without using any chemical with an aim to enhance the anti-oxidant potential of naringenin. The milled naringenin nanoparticles were characterized for their physicochemical properties using scanning electron microscopy (SEM) and X-ray diffraction. Additionally, the effects of milling time and temperature were further assessed on the solubility of crude and milled naringenin samples. The antioxidant potential of milled naringenin was evaluated with various assays such as DHE, DCFDA, and cleaved caspase-3 using SH-SY5Y human neuroblastoma cells. The nanoparticle size of naringenin after milling was confirmed using SEM analysis. Crystalline peaks for milled and crude samples of naringenin also established that both the naringenin forms were in the crystalline form. The solubility of naringenin was enhanced depending on the milling time and temperature. Moreover, crude and milled naringenin were found to be cytocompatible up to doses of 120 μM each for the duration of 24 and 48 h. It was also observed that milled naringenin at the doses of 1, 2, and 5 μM significantly reduced the levels of reactive oxygen species (ROS) generated by H 2 O 2 and exhibited superior ROS scavenging effects as compared to those of crude or un-milled forms of naringenin. Furthermore, milled naringenin at the doses of 1 and 2 μM inhibited H 2 O 2 -induced cell death, as shown by immunofluorescence staining of cleaved caspase-3 and Annexin-V PI flow cytometry analysis. Conclusively, it could be suggested that the size reduction of naringenin using high-energy ball milling techniques substantially enhanced the antioxidant potential as compared to naïve or crude naringenin, which may be attributed to its enhanced solubility due to reduced size.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

Enhanced Antioxidant Effects of Naringenin Nanoparticles Synthesized using the High-Energy Ball Milling Method

Ahmad¹,

Prakash

Khan

et al. 2022

ACS Omega

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“…The brains were collected and homogenized. After centrifugation (3000 rpm, 15 min), the supernatants were separated and stowed at −20 °C and the piperine content was analyzed using the RP-HPLC method and Cmax and AUC was calculated [ 29 ].…”

Section: Methodsmentioning

confidence: 99%

Spanlastics as a Potential Approach for Enhancing the Nose-To-Brain Delivery of Piperine: In Vitro Prospect and In Vivo Therapeutic Efficacy for the Management of Epilepsy

et al. 2023

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The present study delineates the preparation of piperine-loaded spanlastics (PIP-SPL) to improve piperine (PIP) solubility, bioavailability, and permeation through nasal mucosa for intranasal delivery. PIP-SPL was formulated using the thin-film hydration method and optimization was performed using Box–Behnken design (BBD). PIP-SPL optimized formulation (PIP-SPLopt) was characterized for polydispersity index (PDI), vesicle size, entrapment efficiency, zeta potential, and in vitro PIP release. For further evaluation, blood–brain distribution study, transmission electron microscopy (TEM), nasal permeation study, and confocal scanning laser microscopy (CLSM) were performed withal. The PIP-SPLopt presented spherical and sealed shape vesicles with a small vesicle size of 152.4 nm, entrapment efficiency of 72.93%, PDI of 0.1118, and in vitro release of 82.32%. The CLSM study unveiled that the developed formulation has greater permeation of PIP across the nasal mucosa in comparison with the PIP suspension. The blood–brain distribution study demonstrated higher Cmax and AUC0–24h of PIP-SPL via the intranasal route in comparison to PIP-SPL via oral administration. The in vivo study revealed that the PIP-SPL has good antiepileptic potential in comparison with the standard diazepam, which was evinced by seizure activity, neuromuscular coordination by rotarod test, biochemical estimation of oxidative stress markers, and histopathological studies. Furthermore, nasal toxicity study confirm that the developed PIP-SPL formulation is safer for intranasal application. The current investigation corroborated that the prepared spanlastic vesicle formulation is a treasured carrier for the PIP intranasal delivery for the management of epilepsy.

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“…A nanocrystal strategy through the wet milling of naringenin with a co-poloxamer (F127) was also applied and resulted in bioavailability improvement and synovial damage, as well. Oral administration of nanocrystal has increased the cellular uptake and diffusion in CIA-induced RA model [ 66 ].…”

Section: Designed Polyphenolic-loaded Nanocarriers For Inflammation-m...mentioning

confidence: 99%

Modulating Inflammation-Mediated Diseases via Natural Phenolic Compounds Loaded in Nanocarrier Systems

2023

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The global increase and prevalence of inflammatory-mediated diseases have been a great menace to human welfare. Several works have demonstrated the anti-inflammatory potentials of natural polyphenolic compounds, including flavonoid derivatives (EGCG, rutin, apigenin, naringenin) and phenolic acids (GA, CA, etc.), among others (resveratrol, curcumin, etc.). In order to improve the stability and bioavailability of these natural polyphenolic compounds, their recent loading applications in both organic (liposomes, micelles, dendrimers, etc.) and inorganic (mesoporous silica, heavy metals, etc.) nanocarrier technologies are being employed. A great number of studies have highlighted that, apart from improving their stability and bioavailability, nanocarrier systems also enhance their target delivery, while reducing drug toxicity and adverse effects. This review article, therefore, covers the recent advances in the drug delivery of anti-inflammatory agents loaded with natural polyphenolics by the application of both organic and inorganic nanocarriers. Even though nanocarrier technology offers a variety of possible anti-inflammatory advantages to naturally occurring polyphenols, the complexes’ inherent properties and mechanisms of action have not yet been fully investigated. Thus, expanding the quest on novel natural polyphenolic-loaded delivery systems, together with the optimization of complexes’ activity toward inflammation, will be a new direction of future efforts.

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Naringenin nanocrystals for improving anti-rheumatoid arthritis activity

Cited by 24 publications

References 37 publications

Enhanced Antioxidant Effects of Naringenin Nanoparticles Synthesized using the High-Energy Ball Milling Method

Enhanced Antioxidant Effects of Naringenin Nanoparticles Synthesized using the High-Energy Ball Milling Method

Spanlastics as a Potential Approach for Enhancing the Nose-To-Brain Delivery of Piperine: In Vitro Prospect and In Vivo Therapeutic Efficacy for the Management of Epilepsy

Modulating Inflammation-Mediated Diseases via Natural Phenolic Compounds Loaded in Nanocarrier Systems

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