Preparation of β-CD-Ellagic Acid Microspheres and Their Effects on HepG2 Cell Proliferation

Wang, Hongkai; Zhang, Yingxia; Tian, Zhongjing; Ma, Jun; Kang, Meiling; Ding, Chengshi; Ming, Dongfeng

doi:10.3390/molecules22122175

Cited by 24 publications

(26 citation statements)

References 30 publications

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“…The assay was conducted in accordance with the protocol described previously with slight modification [16]. Briefly, for saturated aqueous solution preparation, 5 g of β-CD was dissolved in 200 ml of double-distilled water (DDW).…”

Section: Methodsmentioning

confidence: 99%

“…Furthermore, EA has a short plasma half-life because its oral administration leads to a lactone ring opening by the intestinal microorganism and is rapidly eliminated from the body, which are the main causes of its low bioavailability [15]. Therefore, the preparation of slow-release ellagic acid microspheres could solve these problems [16]. Nanoparticles (NPs) are considered to be the most promising delivery system for compounds with low bioavailability.…”

Section: Introductionmentioning

confidence: 99%

“…β-Cyclodextrin (β-CD) is a cyclodextrin cyclic oligosaccharide produced by cyclodextrin glucose transferase. The formation of inclusion compounds is one of the most important features of β-CD [16]. β-CD is hydrophobic inside and hydrophilic outside; thus, it can form complexes with hydrophobic compounds and enhance the solubility, bioavailability and permeability of such compounds through mucosal tissues [19].…”

Section: Introductionmentioning

confidence: 99%

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Ellagic acid microspheres restrict the growth of Babesia and Theileria in vitro and Babesia microti in vivo

2019

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Background There are no effective vaccines against Babesia and Theileria parasites; therefore, therapy depends heavily on antiprotozoal drugs. Treatment options for piroplasmosis are limited; thus, the need for new antiprotozoal agents is becoming increasingly urgent. Ellagic acid (EA) is a polyphenol found in various plant products and has antioxidant, antibacterial and effective antimalarial activity in vitro and in vivo without toxicity. The present study documents the efficacy of EA and EA-loaded nanoparticles (EA-NPs) on the growth of Babesia and Theileria . Methods In this study, the inhibitory effect of EA, β-cyclodextrin ellagic acid (β-CD EA) and antisolvent precipitation with a syringe pump prepared ellagic acid (APSP EA) was evaluated on four Babesia species and Theileria equi in vitro , and on the multiplication of B. microti in mice. The cytotoxicity assay was tested on Madin-Darby bovine kidney (MDBK), mouse embryonic fibroblast (NIH/3T3) and human foreskin fibroblast (HFF) cell lines. Results The half-maximal inhibitory concentration (IC 50 ) values of EA and β-CD EA on B. bovis , B. bigemina , B. divergens , B. caballi and T. equi were 9.58 ± 1.47, 7.87 ± 5.8, 5.41 ± 2.8, 3.29 ± 0.42 and 7.46 ± 0.6 µM and 8.8 ± 0.53, 18.9 ± 0.025, 11 ± 0.37, 4.4 ± 0.6 and 9.1 ± 1.72 µM, respectively. The IC 50 values of APSP EA on B. bovis , B. bigemina , B. divergens , B. caballi and T. equi were 4.2 ± 0.42, 9.6 ± 0.6, 2.6 ± 1.47, 0.92 ± 5.8 and 7.3 ± 0.54 µM, respectively. A toxicity assay showed that EA, β-CD EA and APSP EA affected the viability of cells with a half-maximal effective concentration (EC 50 ) higher than 800 µM. In the experiments on mice, APSP EA at a concentration of 70 mg/kg reduced the peak parasitemia of B . microti by 68.1%. Furthermore, the APSP EA-atovaquone (AQ) combination showed a higher chemotherapeutic effect than that of APSP EA monotherapy. Conclusions To our knowledge, this is the first study to demonstrate the in vitro and in vivo antibabesial action of EA-NPs and thus supports the use of nanoparticles as an alternative antiparasitic agent. Electronic supplementary material The online version of this article (10.1186/s13071-019-3520-x) contains supplementary ma...

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Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Ellagic acid microspheres restrict the growth of Babesia and Theileria in vitro and Babesia microti in vivo

2019

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“…However, the encapsulation of ellagic acid to enhance its poor solubility combined with an improvement of its controlled delivery was attempted by some research groups [ 148 , 149 ]. In a recent work, Pirzadeh-Naeeni et al reported the nanoencapsulation of ellagic acid in two different biopolymers (schizophyllan and chitin), which were then tested against MCF-7 breast cancer cells [ 150 ].…”

Section: Polyphenolsmentioning

confidence: 99%

Current Perspectives of the Applications of Polyphenols and Flavonoids in Cancer Therapy

et al. 2020

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The development of anticancer therapies that involve natural drugs has undergone exponential growth in recent years. Among the natural compounds that produce beneficial effects on human health, polyphenols have shown potential therapeutic applications in cancer due to their protective functions in plants, their use as food additives, and their excellent antioxidant properties. The possibility of combining conventional drugs—which are usually more aggressive than natural compounds—with polyphenols offers very valuable advantages such as the building of more efficient anticancer therapies with less side effects on human health. This review shows a wide range of trials in which polyphenolic compounds play a crucial role as anticancer medicines alone or in combination with other drugs at different stages of cancer: cancer initiation, promotion, and growth or progression. Moreover, the future directions in applications of various polyphenols in cancer therapy are emphasized.

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“…By following a different preparative procedure, β-CD was again chosen as EA complexing agent in another study [62]. A saturated aqueous β-CD solution was slowly mixed with 125 mg/mL of EA ethanolic solution and stirred for 2 h at rt, then the mixture was filtered and finally freezedried.…”

Section: Ea Inclusion In Cyclodextrins (Cd)mentioning

confidence: 99%

Formulation Strategies to Improve Oral Bioavailability of Ellagic Acid

Zuccari¹,

Baldassari²,

Ailuno³

et al. 2020

Preprint

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Featured Application: An updated description of pursued approaches for efficiently resolving the low bioavailability issue of ellagic acid. Abstract: Ellagic acid, a polyphenolic compound present in fruits and berries, has recently been object of extensive research for its antioxidant activity, which might be useful for the prevention and treatment of cancer, cardiovascular pathologies, and neurodegenerative disorders. Its protective role justifies numerous attempts to include it in functional food preparations and in dietary supplements not only to limit the unpleasant collateral effects of chemotherapy. However, ellagic acid use as chemopreventive agent has been debated because of its poor bioavailability associated to low solubility, limited permeability, first pass effect, and interindividual variability in gut microbial transformations. To overcome these drawbacks, various strategies for oral administration including solid dispersions, micro-nanoparticles, inclusion complexes, selfemulsifying systems, polymorphs have been proposed. Here, we have listed an updated description of pursued micro/nanotechnological approaches focusing on the fabrication processes and the features of the obtained products, as well as on the positive results yielded by in vitro and in vivo studies in comparison to the raw material. The micro/nano-sized formulations here described might be exploited for pharmaceutical delivery of this active, as well as for the production of nutritional supplements or for the enrichment of novel foods.

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Preparation of β-CD-Ellagic Acid Microspheres and Their Effects on HepG2 Cell Proliferation

Cited by 24 publications

References 30 publications

Ellagic acid microspheres restrict the growth of Babesia and Theileria in vitro and Babesia microti in vivo

Ellagic acid microspheres restrict the growth of Babesia and Theileria in vitro and Babesia microti in vivo

Current Perspectives of the Applications of Polyphenols and Flavonoids in Cancer Therapy

Formulation Strategies to Improve Oral Bioavailability of Ellagic Acid

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