Effect of piperine on the bioavailability and pharmacokinetics of emodin in rats

Di, Xin; Wang, Xin; Liu, Youping

doi:10.1016/j.jpba.2015.06.027

Cited by 77 publications

(50 citation statements)

References 17 publications

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“…Interestingly, compared with the limited improvement on MGF, NTR exhibited a strikingly higher shift (301%), which probably occurred because NTR is also modulated by the P-gp transporters and NTR exposure was more dependent on P-gp transporters than MGF, although this hypothesis requires further study. However, the exposure of MGF in rats was significantly decreased by 45.5% and 40% in rats after the concomitant administration of piperine and 1-aminobenzotriazole, which are UGT and CYP450 enzyme inhibitors in vivo at an oral dosage of 30 and 100 mg/kg, respectively, according to previous reports [21,22], and a similar trend was observed for those of C max . Moreover, the AUC of NTR exhibited a downturn after the co-administration of MGF with the UGT and CYP450 enzyme inhibitors.…”

Section: Discussionsupporting

confidence: 80%

Pharmacokinetics of mangiferin and its metabolite—norathyriol, Part 2: Influence of UGT, CYP450, P‐gp, and enterobacteria and the potential interaction in Rhizoma Anemarrhenae decoction with timosaponin B2 as the major contributor

Tian

et al. 2016

BioFactors

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The poor bioavailability of mangiferin (MGF) is a major obstacle on its further development. Aimed to illustrate the underlying mechanism and improve its poor exposure, the compared PK profiles of MGF and norathyriol (NTR) after different MGF preparation were performed: pure MGF, the Rhizoma Anemarrhenae (Zhi-mu) decoction, MGF, and timosaponin B2 (TB-2) combination. Furthermore, the potential contributing factors, including uridine diphosphoglucuronosyltransferase (UGT), cytochrome P450 (CYP450), P-gp, and enterobacterial were investigated by comparing the PK profiles with and without the corresponding inhibitors or in different rat models. After taking MGF, CYP450 and UGT inhibition could decrease MGF and NTR exposure; Pgp inhibition slightly enhanced (48%) MGF exposure, whereas more apparent for the improved NTR exposure (302%); enterobacterial inhibition almost completely stopped the NTR production, but no such effect was observed for MGF. Compared with the limited improvement by the abovementioned inhibition, the MGF and NTR exposure could significantly increase by 11.5-and 5.9-fold in the Zhi-mu decoction compared with the MGF treatment, probably contributed to TB-2 as an absorption enhancer because the MGF and TB-2 combination produced a similar level of improvement on the PK paremeters of MGF and NTR to the herb treatment. Likewise, most of the effects by UGT, CYP450, P-gp, and enterobacteria followed a similar variation tendency between them. Therefore, the poor bioavailability of MGF possibly mainly attributed to its poor membrane permeability, but not transporters or metabolic enzymes, and the compatibility of MGF and TB-2 could probably expand the prospective application of MGF by improving its bioavailability. V C 2016 BioFactors, 42(5): [545][546][547][548][549][550][551][552][553][554][555] 2016

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Section: Discussionsupporting

confidence: 80%

Pharmacokinetics of mangiferin and its metabolite—norathyriol, Part 2: Influence of UGT, CYP450, P‐gp, and enterobacteria and the potential interaction in Rhizoma Anemarrhenae decoction with timosaponin B2 as the major contributor

Tian

et al. 2016

BioFactors

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“…A similar study showed that piperine significantly increased the C max and area under concentration‐time curve (AUC) of emodin and decreased the AUC and C max of emodin glucuronide. However, the detailed mechanisms of the improved bioavailability of emodin need to be further investigated (Di et al ., ). Traditional oral administration would not be the best method of application of emodin because of poor intestinal absorption, fast elimination and low bioavailability in vivo .…”

Section: Pharmacokineticsmentioning

confidence: 97%

Emodin: A Review of its Pharmacology, Toxicity and Pharmacokinetics

Dong

Yin

et al. 2016

Phytotherapy Research

569

365

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Emodin is a natural anthraquinone derivative that occurs in many widely used Chinese medicinal herbs, such as Rheum palmatum, Polygonum cuspidatum and Polygonum multiflorum. Emodin has been used as a traditional Chinese medicine for over 2000 years and is still present in various herbal preparations. Emerging evidence indicates that emodin possesses a wide spectrum of pharmacological properties, including anticancer, hepatoprotective, antiinflammatory, antioxidant and antimicrobial activities. However, emodin could also lead to hepatotoxicity, kidney toxicity and reproductive toxicity, particularly in high doses and with long-term use. Pharmacokinetic studies have demonstrated that emodin has poor oral bioavailability in rats because of its extensive glucuronidation. This review aims to comprehensively summarize the pharmacology, toxicity and pharmacokinetics of emodin reported to date with an emphasis on its biological properties and mechanisms of action. Copyright © 2016 John Wiley & Sons, Ltd.

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“…When curcumin was included in the composite membrane, it would interrupt the formation of the composite membrane. The tensile strengths of all three types of composite membranes were not much different from each other and were within the range of [15][16][17][18][19][20][21][22] MPa. This implied that the amount of curcumin in the range of 100-200 mg slightly affects the tensile strength of the composite membranes.…”

Section: Swelling and Tensile Strengthmentioning

confidence: 99%

Effect of Piperine on Skin Permeation of Curcumin from a Bacterially Derived Cellulose-Composite Double-Layer Membrane for Transdermal Curcumin Delivery

et al. 2018

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Curcumin is a naturally occurring substance with various pharmacological activities. It has not been developed as a drug because of its low bioavailability due to its low solubility and absorption. Piperine is a natural enhancer that is popularly used to increase the absorption of curcumin in oral applications; however, it has not been applied for transdermal curcumin delivery. This study aims to develop a transdermal curcumin delivery system using piperine as a skin permeation enhancer in the form of composite double-layer membrane; the upper layer consisted of curcumin and the lower layer consisted of piperine. The amount of curcumin was fixed, but the amount of piperine varied at three levels from 1.96% to 7.41%. The composite membrane had moderate mechanical strength (15⁻22 MPa) with a good swelling degree (~435%). From an in vitro skin permeation study, piperine had the effect to increase the permeation of curcumin. The permeation rate was related to the amount of piperine. The composite membrane containing piperine at 7.41% could increase the permeation rate of curcumin by about 1.89 times compared with non-piperine contained membrane. Bacterially-derived cellulose containing curcumin and piperine may have the potential for transdermal curcumin delivery in order to improve curcumin's bioavailability.

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Effect of piperine on the bioavailability and pharmacokinetics of emodin in rats

Cited by 77 publications

References 17 publications

Pharmacokinetics of mangiferin and its metabolite—norathyriol, Part 2: Influence of UGT, CYP450, P‐gp, and enterobacteria and the potential interaction in Rhizoma Anemarrhenae decoction with timosaponin B2 as the major contributor

Pharmacokinetics of mangiferin and its metabolite—norathyriol, Part 2: Influence of UGT, CYP450, P‐gp, and enterobacteria and the potential interaction in Rhizoma Anemarrhenae decoction with timosaponin B2 as the major contributor

Emodin: A Review of its Pharmacology, Toxicity and Pharmacokinetics

Effect of Piperine on Skin Permeation of Curcumin from a Bacterially Derived Cellulose-Composite Double-Layer Membrane for Transdermal Curcumin Delivery

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