Pharmaceutical strategies of improving oral systemic bioavailability of curcumin for clinical application

Ma, Zhuang; Wang, Na; He, Haibing; Tang, Xing

doi:10.1016/j.jconrel.2019.10.053

Cited by 260 publications

(138 citation statements)

References 130 publications

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“…The blood plasma bioavailability [24] of ZEN and α-ZEL on different days of the experiment is given in Figure 1. ZEN and its metabolite were determined in both experimental groups.…”

Section: Bioavailability Of Zen and Its Metabolitementioning

confidence: 99%

The Effect of Different Doses of Zearalenone in Feed on the Bioavailability of Zearalenone and Alpha-Zearalenol, and the Concentrations of Estradiol and Testosterone in the Peripheral Blood of Pre-Pubertal Gilts

Zielonka

Gajęcka

Lisieska-Żołnierczyk³

et al. 2020

Toxins

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The objective of this study was to determine the effect of long-term (48 days), per os administration of specific zearalenone (ZEN) doses (20 and 40 μg ZEN/kg BW in experimental groups EI and EII, which were equivalent to 200% and 400% of the upper range limit of the no-observed-adverse-effect-level (NOAEL), respectively) on the bioavailability of ZEN and the rate of changes in estradiol and testosterone concentrations in the peripheral blood of pre-pubertal gilts. ZEN and α-ZEL levels were similar until day 28. After day 28, α-ZEL concentrations increased significantly in group EI, whereas a significant rise in ZEN levels was noted in group EII. The presence of estradiol in peripheral blood plasma was not observed until day 20 of the experiment. Spontaneous secretion of estradiol was minimal, and it was determined at very low levels of up to 10 pg/mL in EI and EII groups. Testosterone concentrations ranged from 4 to 9 ng/mL in all groups. A decrease in the concentrations of both analyzed hormones was reported in the last stage of the experiment. The results of the experiment indicate that: (i) The bioavailability of ZEN in peripheral blood has low diagnostic value, (ii) exposure to low doses of ZEN induces minor changes in the concentrations of the analyzed hormones, which could lead to situational supraphysiological hormone levels and changes in endogenous hormonal balance.

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“…The blood plasma bioavailability [24] of ZEN and α-ZEL on different days of the experiment is given in Figure 1. ZEN and its metabolite were determined in both experimental groups.…”

Section: Bioavailability Of Zen and Its Metabolitementioning

confidence: 99%

The Effect of Different Doses of Zearalenone in Feed on the Bioavailability of Zearalenone and Alpha-Zearalenol, and the Concentrations of Estradiol and Testosterone in the Peripheral Blood of Pre-Pubertal Gilts

Zielonka

Gajęcka

Lisieska-Żołnierczyk³

et al. 2020

Toxins

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“…OB refers to the percentage and rate of the release and absorption of active ingredients into the systemic blood circulation and is an important pharmacokinetic index of oral drugs [25]. It is also an important index to objectively evaluate the intrinsic quality of oral drugs [26], which is particularly important in the drug administration of most oral Chinese herbal formulas [27]. DL is defined as a complex balance of structural features and various molecular properties, which determine whether the particular molecule is similar to the known drugs [26].…”

Section: Pharmacokinetic Prediction Of Cddmentioning

confidence: 99%

Identification of the Active Constituents and Significant Pathways of Cangfu Daotan Decoction for the Treatment of PCOS Based on Network Pharmacology

Tang

Wang

et al. 2020

Evidence-Based Complementary and Alternative Medicine

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Background. Polycystic ovary syndrome (PCOS) is the most common female endocrine disease. Cangfu Daotan Decoction (CDD) can effectively relieve the clinical symptoms of PCOS patients. Methods. To explore the active ingredients and related pathways of CDD for treating PCOS, a network pharmacology-based analysis was carried out. The active ingredients of CDD and their potential targets were obtained from the TCM system pharmacology analysis platform. The obtained PCOS-related genes from OMIM and GeneCards were imported to establish protein-protein interaction networks in STRING. Finally, GO analysis and significant pathway analysis were conducted with the RStudio (Bioconductor) database. Results. A total of 111 active compounds were obtained from 1433 ingredients present in the CDD, related to 118 protein targets. In addition, 736 genes were found to be closely related to PCOS, of which 44 overlapped with CDD and were thus considered therapeutically relevant. Pathway enrichment analysis identified the AGE-RAGE signalling pathway in diabetic complications, endocrine resistance, the IL-17 signalling pathway, the prolactin signalling pathway, and the HIF-1 signalling pathway. Moreover, PI3K-Akt, insulin resistance, Toll-like receptor, MAPK, and AGE-RAGE were related to PCOS and treatment. Conclusions. CDD can effectively improve the symptoms of PCOS, and our network pharmacological analysis lays the foundation for future clinical research.

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“…native from southern Asia (Willenbacher et al, 2019 ). In turmeric, curcumin is identified as the major active curcuminoids, as compared to its two dimethoxy derivatives, dimethoxycurcumin (DMC, one -OMe at the outer phenol rings is removed) and bis-demethoxycurcumin (BMC, two -OMes are removed), with the ratio being 77:3:17 (Ma et al, 2019 ). Over the past few decades, a plenty of curcumin bioactivities have been revealed, including anti-cancer (Nagaraju et al, 2019 ; Yedjou et al, 2019 ), anti-inflammation (Farhood et al, 2019 ), antioxidation (Abrahams et al, 2019 ), anti-microbe (Sharifi et al, 2020 ), anti-hepatotoxicity (Fujiwara et al, 2008 ) and anti-Alzheimer (Bhat et al, 2019 ), and this wide range of biological effects has been attributed to essential molecules related to human diseases, such as cyclooxygenase-2 (COX-2), matrix metallopeptidases (MMPs), glutathione, protein kinase C, ATPase, NF-κB, activator protein 1 (AP-1), P-glycoprotein (P-gp), multidrug resistance-associated protein 1 (MRP-1), multidrug resistance-associated protein 2 (MRP-2), and cyclin D1 (Lev-Ari et al, 2006 ; Stridh et al, 2010 ; Kao et al, 2011 ; Sreenivasan et al, 2012 ; Mishra et al, 2015 ; Ge et al, 2016 ; Lopes-Rodrigues et al, 2016 ; Seo et al, 2016 ; Zhu et al, 2016 ).…”

Section: Introductionmentioning

confidence: 99%

“…Although organic solvents, oils and surfactants have been suggested to produce highly soluble solutions of curcumin, their cytotoxic effects exert additional considerations in the development of curcumin-originated medications (Tønnesen et al, 2002 ). Moreover, the fact that curcumin is highly sensitive to light and metabolism of curcumin is under the control of several GI factors, such as pH, gastric acid, bile, and digestive enzymes (Ma et al, 2019 ), further hampers its therapeutic application (Rutz et al, 2019 ).…”

Section: Introductionmentioning

confidence: 99%

Application of Functional Biocompatible Nanomaterials to Improve Curcumin Bioavailability

Shi

et al. 2020

Front. Chem.

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Curcumin is a lipophilic natural product extracted from turmeric and commonly used as a dietary spice. Being multi-functional, curcumin has been proposed in the prevention and treatment of a broad spectrum of diseases. However, due to unsatisfactory aqueous solubility and hence low bioavailability, clinical application of curcumin has been greatly restrained. To break these limitations, biocompatible nanoformulation, such as liposomes, nanoparticles, micelles, nanoemulsions and conjugates has been employed as alternatives to improve in vivo delivery of curcumin. In this scenario, in order to enhance bioavailability of curcumin, the choice of effective molecules as facilitators is of prominence. In this review, we focus on functional biocompatible materials, including polymers, protein molecules, polysaccharide, surface stabilizers and phospholipid complexes, and decipher their potential applications as how they assist to promote medicinal performance of curcumin.

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Pharmaceutical strategies of improving oral systemic bioavailability of curcumin for clinical application

Cited by 260 publications

References 130 publications

The Effect of Different Doses of Zearalenone in Feed on the Bioavailability of Zearalenone and Alpha-Zearalenol, and the Concentrations of Estradiol and Testosterone in the Peripheral Blood of Pre-Pubertal Gilts

The Effect of Different Doses of Zearalenone in Feed on the Bioavailability of Zearalenone and Alpha-Zearalenol, and the Concentrations of Estradiol and Testosterone in the Peripheral Blood of Pre-Pubertal Gilts

Identification of the Active Constituents and Significant Pathways of Cangfu Daotan Decoction for the Treatment of PCOS Based on Network Pharmacology

Application of Functional Biocompatible Nanomaterials to Improve Curcumin Bioavailability

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