Comparative bio-accessibility, bioavailability and bioequivalence of quercetin, apigenin, glucoraphanin and carotenoids from freeze-dried vegetables incorporated into a baked snack versus minimally processed vegetables: Evidence from in vitro models and a human bioavailability study

Pérez-Moral, Natalia; Saha, Shikha; Philo, Mark; Hart, Dave J.; Winterbone, Mark S.; Hollands, Wendy J; Spurr, Mike; Bows, John R.; Velpen, Vera van der; Kroon, Paul A.; Curtis, Peter J.

doi:10.1016/j.jff.2018.07.035

Cited by 20 publications

(16 citation statements)

References 35 publications

(35 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…It has poor aqueous solubility and belongs to BCS-II class category ( Huang et al, 2016 ). Due to poor aqueous solubility, their bioavailability is limited (~7.1%) and led to poor therapeutic efficacy after single-dose oral administration in the rat ( Perez-Moral et al, 2018 , Elhennawy and Lin, 2018 ).…”

Section: Introductionmentioning

confidence: 99%

Bioactive Apigenin loaded oral nano bilosomes: Formulation optimization to preclinical assessment

Zafar

Alruwaili

Imam

et al. 2021

Saudi Pharmaceutical Journal

View full text Add to dashboard Cite

Aim Diabetic (type-2) is a metabolic disease characterized by increased blood glucose level from the normal level. In the present study, apigenin (AG) loaded lipid vesicles (bilosomes: BIL) was prepared, optimized and evaluated for the oral therapeutic efficacy. Experimental AG-BIL was prepared by a thin-film evaporation method using cholesterol, span 60 and sodium deoxycholate. The prepared formulation was optimized by 3-factor and 3-level Box-Behnken design using particle size, entrapment efficiency and drug release as a response. The selected formulation further evaluated for ex-vivo permeation, in vivo pharmacokinetic and pharmacodynamics study. Results The optimized AG bilosomes (AG-BILopt) has shown the vesicle size 183.25 ± 2.43 nm, entrapment efficiency 81.67 ± 4.87%. TEM image showed a spherical shape vesicle with sharp boundaries. The drug release study revealed a significant enhancement in AG release (79.45 ± 4.18%) from AG-BILopt as compared to free AG-dispersion (25.47 ± 3.64%). The permeation and pharmacokinetic studies result revealed 4.49 times higher flux and 4.67 folds higher AUC 0-t than free AG-dispersion. The antidiabetic activity results showed significant (P < 0.05) enhancement in therapeutic efficacy than free AG-dispersion. The results also showed marked improvement in biochemical parameters. Conclusion Our findings suggested, the prepared apigenin loaded bilosomes was found to be an efficient delivery in the therapeutic efficacy in diabetes.

show abstract

Section: Introductionmentioning

confidence: 99%

Bioactive Apigenin loaded oral nano bilosomes: Formulation optimization to preclinical assessment

Zafar

Alruwaili

Imam

et al. 2021

Saudi Pharmaceutical Journal

View full text Add to dashboard Cite

show abstract

“…Apigenin is present in many kinds of food, such as fruit, seasonings and vegetables. Apigenin is a part of the average daily diet (7)(8)(9). It has been shown that apigenin can significantly suppress malignant cell growth in cultivated cells and in vivo malignant models (10)(11)(12)(13).…”

Section: Introductionmentioning

confidence: 99%

Apigenin induces apoptosis and counteracts cisplatin‑induced chemoresistance via Mcl‑1 in ovarian cancer cells

Ding

Yao

et al. 2020

Exp Ther Med

View full text Add to dashboard Cite

Ovarian cancer (OC) is one of the prominent causes of mortality in female patients diagnosed with gynecologic malignancies. While it has previously been demonstrated that apigenin inhibits cell growth in colon and breast cancer cells, the effect of apigenin in OC cells is not fully understood. Therefore, the aim of the present study was to investigate the impact of apigenin on cell death and resistance to cisplatin in OC cells. It was found that apigenin inhibited proliferation, hindered cell cycle progression and promoted SKOV3 cell apoptosis. Moreover, these effects were also observed in cisplatin-resistant SKOV3/DDP cells. Furthermore, apigenin reduced the mitochondrial transmembrane potential, and elevated the ratios of cleaved caspase-3/caspase-3 and Bax/Bcl-2 in the two cell types. Reverse transcription-quantitative PCR and western blotting results demonstrated that apigenin significantly downregulated Mcl-1 at the transcriptional and translational levels in SKOV3 and SKOV3/DDP cells, which was responsible for its cytotoxic functions and chemosensitizing effects. Collectively, the present results identified the impact of apigenin on OC cell death and resistance to cisplatin, and the potential molecular mechanisms. However, additional studies are required to further elucidate the underlying mechanisms.

show abstract

“…It has been proposed as practically insoluble/poorly soluble in water (solubility: 15.60 µg/ml at ambient temperature) and aqueous buffers (Zhang et al, 2012, Shakeel et al, 2017, Shakeel et al, 2018). Its oral bioavailability in rats and humans has been reported as very low (Elhennawy and Lin, 2018, Perez-Moral et al, 2018). Upon single dose administration of APG in rats, its oral bioavailability was obtained as very low i.e.…”

Section: Introductionmentioning

confidence: 99%

Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques

Alshehri

Shakeel

Ibrahim

et al. 2019

Saudi Pharmaceutical Journal

View full text Add to dashboard Cite

Apigenin (APG) is a poorly soluble bioactive compound/nutraceutical which shows poor bioavailability upon oral administration. Hence, the objective of this research work was to develop APG solid dispersions (SDs) using different techniques with the expectation to obtain improvement in its in vitro dissolution rate and in vivo bioavailability upon oral administration. Different SDs of APG were prepared by microwave, melted and kneaded technology using pluronic-F127 (PL) as a carrier. Prepared SDs were characterized using “thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), Fourier transform infra-red (FTIR) spectrometer, powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM)”. After characterization, prepared SDs of APG were studied for in vitro drug release/dissolution profile and in vivo pharmacokinetic studies. The results of TGA, DSC, FTIR, PXRD and SEM indicated successful formation of APG SDs. In vitro dissolution experiments suggested significant release of APG from all SDs (67.39–84.13%) in comparison with control (32.74%). Optimized SD of APG from each technology was subjected to in vivo pharmacokinetic study in rats. The results indicated significant improvement in oral absorption of APG from SD prepared using microwave and melted technology in comparison with pure drug and commercial capsule. The enhancement in oral bioavailability of APG from microwave SD (319.19%) was 3.19 fold as compared with marketed capsule (100.00%). Significant enhancement in the dissolution rate and oral absorption of APG from SD suggested that developed SD systems can be successfully used for oral drug delivery system of APG.

show abstract

Comparative bio-accessibility, bioavailability and bioequivalence of quercetin, apigenin, glucoraphanin and carotenoids from freeze-dried vegetables incorporated into a baked snack versus minimally processed vegetables: Evidence from in vitro models and a human bioavailability study

Abstract: Graphical abstract

Cited by 20 publications

References 35 publications

Bioactive Apigenin loaded oral nano bilosomes: Formulation optimization to preclinical assessment

Bioactive Apigenin loaded oral nano bilosomes: Formulation optimization to preclinical assessment

Apigenin induces apoptosis and counteracts cisplatin‑induced chemoresistance via Mcl‑1 in ovarian cancer cells

Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques

Contact Info

Product

Resources

About