Improved solubility and oral bioavailability of apigenin via Soluplus/Pluronic F127 binary mixed micelles system

Zhang, Zhenhai; Cui, Changchang; Wei, Fang; Lv, Huixia

doi:10.1080/03639045.2017.1313857

Cited by 55 publications

(30 citation statements)

References 26 publications

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“…These challenges could be overcomed by new "lipid-based nano-encapsulation approaches" for targeted delivery of these functional compounds (Esfanjani, Assadpour, & Jafari, 2018). Innovative technologies such as nanocrystals, lipid-based nanoparticles including liposomes, phytosomes, micelles, solid lipid nanoparticles, microemulsions, and nanoemulsions, and solubility enhancing agents such as cyclodextrin have been reported for improvement of beneficial effects of celery's compounds (Dang et al, 2014;Ding, Zhang, et al, 2014;Huang et al, 2016;Khan, Saraf, & Saraf, 2016;Kim, Cho, & Park, 2016;Luo et al, 2019;Mahalapbutr et al, 2019;Shi, Zhao, Firempong, & Xu, 2016;Shin et al, 2018;Telange et al, 2017;Wu, Li, Yue, Zhang, & Yunusi, 2018;Wu et al, 2017;Zhai et al, 2013;Zhang, Huang, Liu, Gao, & Qian, 2013;Zhang, Cui, Wei, & Lv, 2017;Zhao, Wang, & Li, 2016). The effects of celery on metabolic syndrome are shown in Figure 2.…”

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confidence: 99%

Beneficial effects of celery (Apium graveolens) on metabolic syndrome: A review of the existing evidences

Hedayati

Naeini

Mohammadinejad

et al. 2019

Phytotherapy Research

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The metabolic syndrome (MetS) is a cluster of multiple conditions that includes hypertension, dyslipidemia, abdominal obesity, and hyperglycemia disorders. Most studies revealed that the MetS is accompanied with an increased risk for cardiovascular disease, Type 2 diabetes mellitus, and insulin resistance. It can be said that, in treating or preventing the MetS and its components, lifestyle adjustment and weight loss have a vital role. According to various studies, among natural compounds, celery (Apium graveolens) is one of the most important sources of phytochemicals such as phenolic acids, flavones, flavonols, and antioxidants such as vitamin C, beta‐carotene (Provitamin A), and manganese. These antioxidants have a role in decreasing the oxidative damage. The phytochemicals in celery decrease the activity of proinflammatory cytokines and prevent inflammation. Also, flavonoids in celery suppress cardiovascular inflammation. Oxidative stress and inflammation in the blood stream are the main risk factors in increasing cardiovascular disease, especially atherosclerosis. Celery phthalides leads to expanding of smooth muscle in the blood vessels and lower blood pressure. As a result, the most active ingredients in celery (A. graveolens (have shown hypolipidemic, antidiabetic, and hypotensive properties. In this review, we summarized the mechanisms underlying the protective effects of celery components on insulin action, glucose, lipid metabolism, and blood pressure.

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mentioning

confidence: 99%

Beneficial effects of celery (Apium graveolens) on metabolic syndrome: A review of the existing evidences

Hedayati

Naeini

Mohammadinejad

et al. 2019

Phytotherapy Research

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“…In addition, the supercritical-fluid technique also exists many problems including large equipment investment, wasted energy, and lower productivity (Zhe et al, 2007;Zhao et al, 2013), and so on. Moreover, the apigenin-loaded liposomes (Banerjee et al, 2015;Banerjee et al, 2017;Jin et al, 2017), the apigenin-loaded ethosome (Shen et al, 2014), the apigenin-loaded micelles (Zhai et al, 2013;Zhang et al, 2017) and the apigenin-loaded emulsions (Kim et al, 2016) of small particle size are also successfully prepared, but these nanoformulation strategies may have the problems of low entrapment efficiency and poor stability. The liquid antisolvent precipitation (LAP) technique is believed to be a promising technique in preparing nano/ micro particles in recent years, compared with other micronization technologies, its process is relatively simple, easy to operate, lower cost, high yield, and has the potential to be applied in the pharmaceutical industry (Zu et al, 2013;Yadav & Kumar, 2014).…”

Section: Introductionmentioning

confidence: 99%

Preparation, characterization and antitumor activity evaluation of apigenin nanoparticles by the liquid antisolvent precipitation technique

Wei

Wang

et al. 2017

Drug Delivery

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The present work aimed to apply the liquid antisolvent precipitation (LAP) method for preparing the apigenin nanoparticles and thereby improving the solubility and bioavailability of apigenin. The different experimental parameters on particle size were optimized through central composite design (CCD) using the Design-Expert V R software. Under the optimum conditions, the particle size of the apigenin nanosuspension was about 159.2 nm. In order to get apigenin nanoparticles, the freeze-drying method was selected and the mannitol was used as a cryoprotectant. Then the solid state properties of the apigenin nanoparticles were investigated using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), thermo gravimetric (TG), and X-ray diffraction (XRD). The results obtained displayed that the apigenin nanoparticles exhibited near-spherical shape and could be transformed into an amorphous form. In addition, the dissolving test, the bioavailability in rats, and the antitumor activity were also studied. The experimental results showed that the solubility of the apigenin nanoparticles were about 29.61 times and 64.81 times of raw apigenin in artificial gastric juice and in artificial intestinal juice, respectively, and the apigenin nanoparticles showed higher dissolution rates compared to raw apigenin, and was about 6.08 times and 6.14 times than that of raw apigenin in artificial gastric juice and in artificial intestinal juice. The oral bioavailability of apigenin nanoparticles was about 4.96 times higher than that of the raw apigenin, but the apigenin nanoparticles had no toxic effect on the organs of rats. In addition, the apigenin nanoparticles had a higher inhibition to HepG2 cells by lower IC50 than that of raw apigenin. ARTICLE HISTORY

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“…Freshly prepared 200 ml of release medium containing phosphate‐buffered saline (PBS, pH 7.4, 37°C) with 0.5% (w/v) Tween 80, and the whole process was under sink condition. At predetermined time intervals (1, 2, 3, 6, 8, 10, 20, 30, 40 and 60 h after test), triplicate suspensions (0.5 ml) were withdrawn from the release medium and filtered through a 0.22‐μm microporous membrane for analysis and replaced with the same volume of fresh medium . The filtrates obtained at different time intervals were analysed by HPLC method.…”

Section: Methodsmentioning

confidence: 99%

“…At predetermined time intervals (1, 2, 3, 6, 8, 10, 20, 30, 40 and 60 h after test), triplicate suspensions (0.5 ml) were withdrawn from the release medium and filtered through a 0.22-lm microporous membrane for analysis and replaced with the same volume of fresh medium. [22] The filtrates obtained at different time intervals were analysed by HPLC method. The cumulative amount of BAI released from the micelles was plotted against time.…”

Section: In Vitro Release Studymentioning

confidence: 99%

Enhancing the oral bioavailability of baicalein via Solutol® HS15 and Poloxamer 188 mixed micelles system

Shen

Liu

Zhang

et al. 2019

Journal of Pharmacy and Pharmacology

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Objectives To increase the solubility of baicalein (BAI) by preparing BAI‐micelles (BAI‐M) with Solutol HS15 (HS15) and Poloxamer 188 (F68), thereby improving its oral bioavailability. Methods Baicalein micelles were prepared with HS15 and F68 by thin‐film dispersion method and optimized by central composite design (CCD) approach. Physicochemical, in vitro release, Caco‐2 cell transport and pharmacokinetic studies of BAI‐M were performed. Key findings The optimal formulation showed spherical shape by characterization of the transmission electron microscope with average small size (23.14 ± 1.46 nm) and high entrapment efficiency (92.78±0.98%) and drug loading (6.45±1.54%). The in vitro release study of BAI‐M showed a significantly sustained release pattern compared with free BAI. Caco‐2 cell transport study demonstrated that high permeability of BAI was achieved after loading it into micelles. Meanwhile, pharmacokinetics study of BAI‐M showed a 3.02‐fold increase in relative oral bioavailability compared with free BAI. Conclusions Based on our findings, we concluded that HS15 can be used as a carrier in this drug delivery system that includes F68, and BAI‐M has great potential in improving solubility and oral bioavailability.

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Improved solubility and oral bioavailability of apigenin via Soluplus/Pluronic F127 binary mixed micelles system

Cited by 55 publications

References 26 publications

Beneficial effects of celery (Apium graveolens) on metabolic syndrome: A review of the existing evidences

Beneficial effects of celery (Apium graveolens) on metabolic syndrome: A review of the existing evidences

Preparation, characterization and antitumor activity evaluation of apigenin nanoparticles by the liquid antisolvent precipitation technique

Enhancing the oral bioavailability of baicalein via Solutol® HS15 and Poloxamer 188 mixed micelles system

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