Stability and solubility enhancement of ellagic acid in cellulose ester solid dispersions

Li, Bin; Harich, Kim; Wegiel, Lindsay A.; Taylor, Lynne S.; Edgar, Kevin J.

doi:10.1016/j.carbpol.2012.10.051

Cited by 68 publications

(43 citation statements)

References 36 publications

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“…This low solubility is partly due to its high degree of crystallinity, which is directly related to its planar and symmetrical structure and the hydrogen-bonding network formed in the crystal (Li, Harich, Wegiel, Taylor, & Edgara, 2013). Indeed, previous animal studies identified the low solubility of EA in aqueous media as a major drawback in EA absorption (Daniel, Ratnayake, Kinstle, & Stoner, 1991) as well as its ability to bind the intestinal epithelium (Whitley, Sweet, & Walle, 2006).…”

Section: Discussionmentioning

confidence: 97%

Identifying the limits for ellagic acid bioavailability: A crossover pharmacokinetic study in healthy volunteers after consumption of pomegranate extracts

González‐Sarrías

Garcı́a-Villalba

Núñez‐Sánchez

et al. 2015

Journal of Functional Foods

136

100

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Available online A B S T R A C TEllagic acid (EA) is a polyphenol that must be released from the non-bioavailable ellagitannins in pomegranates, walnuts or strawberries to be absorbed. To estimate whether EA bioavailability could be improved after consumption of a high free EA amount, we conducted a crossover pharmacokinetic study in healthy volunteers that consumed two pomegranate extracts providing either 130 mg punicalagin+524 mg EA (PE-1) or 279 mg punicalagin+25 mg EA (PE-2).Targeted metabolomics (UPLC-ESI-qTOF-MS/MS) identified plasma free EA but not phase-II conjugates. EA pharmacokinetics showed high interindividual variability. Cmax ranged from 12 to 360 nM (PE-1: 74.8 ± 54.4 nM; PE-2: 64.1 ± 76.8 nM). In vitro digestion supported in vivo results. EA bioavailability was limited by the ellagitannin, pH and protein environment. A higher free EA intake does not enhance its bioavailability but promotes urolithin production. Bioavailability of EA, as the unchanged fraction that reaches the systemic circulation, is not as low as previously thought.

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Section: Discussionmentioning

confidence: 97%

Identifying the limits for ellagic acid bioavailability: A crossover pharmacokinetic study in healthy volunteers after consumption of pomegranate extracts

González‐Sarrías

Garcı́a-Villalba

Núñez‐Sánchez

et al. 2015

Journal of Functional Foods

136

100

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“…Recent studies have shown that EA have potential biological activity. Nevertheless, its low bioavailability and low average individual consumption (around 343 mg EA per year) are great challenges for its beneficial functions (21). The nanocarriers can increase the bioavailability of poorly bioavailable drugs due to their specialized uptake mechanism (22) dependent on preparation process and the composition of SLNs (23).…”

Section: Discussionmentioning

confidence: 99%

Enhanced Anti-Cancer Capability of Ellagic Acid Using Solid Lipid Nanoparticles (SLNs)

et al. 2018

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Background: Ellagic acid (EA) is a polyphenol, whose anti-cancer properties have been demonstrated in several cancer studies, but the poor water solubility and low bioavailability have limited its therapeutic potential. Objectives: The present study proposed to develop solid lipid nanoparticles (SLNs) as a delivery system for improving the anticancer capability of EA on prostate cancer cell line. Methods: EA-loaded SLNs were prepared by hot homogenization technique and characterized by different techniques. Cytotoxicity of EA and EA-loaded SLNs on prostate cancer cell line (PC3) was evaluated by 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay, and nucleus condensation, or chromatin fragmentation (the signs of apoptosis) were studied by 4'-6-diamidino-2-phenylindole (DAPI) staining. The expression of B-cell lymphoma 2 (Bcl-2) and Bcl-2-associated X protein (Bax), which are involved in apoptosis, were evaluated by quantitative reverse transcription polymerase chain reaction (qRT-PCR). Results:The nanoparticles with appropriate characteristics (particle size of 96 nm and Encapsulation Efficiency of 88%) were prepared. The in vitro drug release profile showed a burst release in the first hours and followed by a sustained EA release until 72 hours. EA-loaded SLNs displayed a good stability for 4 weeks of storage at 4 -8°C. Cytotoxicity evaluations demonstrated that EA-loaded SLNs prevented prostate cancer cells growth in a low IC50 value compared to the EA. The results of qRT-PCR demonstrated that EA causes up-regulation of Bax and this regulation intensified when EA was loaded into SLNs, but there was no punctual correlation between the EA and EA-loaded SLNs in down-regulation of Bcl-2. Conclusions:The results strengthen our hope that loading EA into SLNs could possibly overcome the therapeutic limitations of EA and make it more effective in prostate cancer therapy.

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“…But almost all the newly discovered drugs are poorly water soluble or lipophilic. The oral deliveries of such drugs are frequently associated with low bioavailability, high intra and inter subject variability 1,2,3 . In order to overcome these problems of poor solubility, many techniques are adopted these days.…”

Section: Introductionmentioning

confidence: 99%

Improved Solubility and Dissolution Release Profile of Lurasidone by Solid Self-Nanoemulsifying Drug Delivery System

Dondapati¹,

Srimathkandala²,

Sanka³

et al. 2016

Analytical Chemistry Letters

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The purpose of the study was to investigate self-nanoemulsifying drug delivery system (SNEDDS) as potential delivery system for poorly water soluble drug Lurasidone (LUR). SNEDDS was formulated using oil (Anise oil) surfactant (Tween ® 80), and co-surfactant (Polyethyleneglycol-600). Z-average size, PDI and in-vitro drug release were considered to screen and optimize the composition of liquid-SNEDDS. Following emulsification, the optimized formulation was selected to have the smallest mean particle size and highest absolute zeta potential, which would yield stable emulsion. Scanning electron microscopy, X-ray powder diffraction studies confirmed that there was no crystalline drug in Solid-SNEDDS. Fourier transform infrared (FTIR) spectroscopy study revealed that there was no measurable chemical interaction of drug with the carrier. There was no significance difference in zeta average, zeta potential, and release profile of developed formulation before and after stability study. Both Liquid-SNEDDS and solid-SNEDDS showed improved invitro drug release than the pure drug. This paper provides an overview of the SNEDDS of LUR as a promising alternative to improve solubility and dissolution release profile. The results suggested that the SNEDDS could be used as an effective oral dosage form to improve the oral delivery of poorly water soluble drug LUR.

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Stability and solubility enhancement of ellagic acid in cellulose ester solid dispersions

Cited by 68 publications

References 36 publications

Identifying the limits for ellagic acid bioavailability: A crossover pharmacokinetic study in healthy volunteers after consumption of pomegranate extracts

Identifying the limits for ellagic acid bioavailability: A crossover pharmacokinetic study in healthy volunteers after consumption of pomegranate extracts

Enhanced Anti-Cancer Capability of Ellagic Acid Using Solid Lipid Nanoparticles (SLNs)

Improved Solubility and Dissolution Release Profile of Lurasidone by Solid Self-Nanoemulsifying Drug Delivery System

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