Oral pharmacokinetic interaction of ester rich fruit juices and pharmaceutical excipients with tenofovir disoproxil fumarate in male Wistar rats

Shailender, Joseph; Ravi, Punna Rao; Saha, Paramita; Myneni, Srividya

doi:10.1080/00498254.2016.1269375

Cited by 6 publications

(3 citation statements)

References 37 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…As TDF is a substrate of Pgp, studies were done to determine whether ester-rich fruit juices increase its bioavailability and intestinal absorption. Strawberry juice extract increased TDF intestinal absorption in Caco-2 cell lines to 67%, whereas grapefruit and cranberry juice extracts increased TDF bioavailability by 97% and 24% in an in vivo rat study (Van Gelder et al, 1999;Shailender et al, 2017). Additional investigation needs to be done to determine whether this effect is also seen in humans.…”

Section: Effect Of Food Intake On Tdf Bioavailabilitymentioning

confidence: 98%

Factors Contributing to the Antiviral Effectiveness of Tenofovir

Murphy

Valentovic

2017

J Pharmacol Exp Ther

View full text Add to dashboard Cite

Over 1 million people in the United States are living with human immunodeficiency virus (HIV), which may progress to AIDS. The use of antiviral therapy has successfully controlled the rate of viral growth in patients. Antiviral agents improve the quality of life and reduce the potential for spreading HIV; HIV is currently considered a chronic disease provided patients are compliant with their antiviral medications. Tenofovir is a nucleoside transcriptase inhibitor that prevents viral replication and is approved for treatment of HIV and chronic hepatitis B infection. Tenofovir is an antiretroviral drug used alone and in combination with other nucleoside reverse-transcriptase inhibitor agents to lower viral load in HIV patients. Tenofovir is administered as a prodrug to increase bioavailability. The prodrug forms of tenofovir are tenofovir disoproxil fumarate, approved in 2001, and tenofovir alafenamide, approved in 2016. Tenofovir is extensively used in controlling HIV, as it is administered once daily, allowing for good compliance. This minireview discusses the impact of food, age, and drug transporters on tenofovir absorption and clearance. The changes in dosing that are needed in the presence of renal impairment, which is a common occurrence with HIV chronic disease progression, will also be discussed. The potential special conditions occurring with fixed-combination doses containing tenofovir will also be reviewed, including the use of cobicistat, a cytochrome P450 3A4 inhibitor. The short review also addresses some newer preparations using niosomes to improve tenofovir absorption and delivery to the target cells.

show abstract

Section: Effect Of Food Intake On Tdf Bioavailabilitymentioning

confidence: 98%

Factors Contributing to the Antiviral Effectiveness of Tenofovir

Murphy

Valentovic

2017

J Pharmacol Exp Ther

View full text Add to dashboard Cite

show abstract

“…Grapefruit also helps with atherosclerosis. Grapefruit juice has exceptional antibacterial, antifungal, and antiviral capabilities [19]. In Japan, experiments on mice showed that tumor growth stopped after mice were being injected under the skin with grapefruit extract.…”

Section: Grapefruit (Citrus Paradisi)mentioning

confidence: 99%

Phytotherapy and Liver Disease

Čalkić¹

2019

Liver Cirrhosis - Debates and Current Challenges

View full text Add to dashboard Cite

Hepatoprotective agents are medicines or dietary supplements that are used as an adjunct to the treatment of acute and chronic viral hepatitis, liver cirrhosis, hepatocellular carcinoma prevention, as well as other liver diseases. Experiments on animals and cell cultures have shown that natural compounds can alleviate and prevent pathological changes in the liver. In the past few years, considerable attention has been paid to medicinal herbs with hepatoprotective, antioxidant, and immune properties. The plants contain numerous phytochemicals, including polyphenols, phenolic acids, coumarins, styles, tannins, lignans, and lignins. These compounds include silymarin, curcumin, picroside, kutkoside, phyllanthin, hypophyllanthin, glycyrrhizin, glycyrrhizin, berberine, luteolin, quercetin, coumarin derivatives (4-methylumbelliferone), and others. Many studies have been aimed at collecting data on some types of edible plants and fruits (grapefruit, cranberries, grapes, beets, cacti, chamomile, spirulina, propolis) that have shown hepatoprotective effects.

show abstract

“…For example, surfactants are used to solubilize hydrophobic drugs, methylcellulose can be used to prepare drug suspensions or added to tablets as a disintegrating agent, and cyclodextrin can be used to improve drug stability or control drug release [ 5 ]. However, not all PEs are “inactive”, and some are reported to affect the activity of metabolic enzymes, such as cytochrome P450 (CYP450) 3A4/5 (CYP3A4/5), CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP1A2, and UGT1A1 [ 6 , 7 , 8 , 9 , 10 ], or drug transporters, such as P-gp, BCRP, MRP2, and OATP1A2/2B1 [ 11 , 12 , 13 , 14 ]. For example, Martin and colleagues investigated the impact of 23 commonly used excipients (10 polymers and 13 surfactants) on CYP2E1, CYP3A4, CYP3A5, CYP2C9, CYP2C19, CYP1A2, and CYP2D6 using baculosome-derived CYP450 enzymes across a range of concentrations [ 10 ].…”

Section: Introductionmentioning

confidence: 99%

Assessing CYP2C8-Mediated Pharmaceutical Excipient-Drug Interaction Potential: A Case Study of Tween 80 and Cremophor EL−35

Wen

Zhang

et al. 2021

Pharmaceutics

View full text Add to dashboard Cite

Pharmaceutical excipients (PEs) are substances included in drug formulations. Recent studies have revealed that some PEs can affect the activity of metabolic enzymes and drug transporters; however, the effects of PEs on CYP2C8 and its interaction potential with drugs remain unclear. In this study, we evaluated the effects of Tween 80 and EL−35 on CYP2C8 in vitro and further investigated their impacts on the PK of paclitaxel (PTX) in rats after single or multiple doses. The in vitro study indicated that Tween 80 and EL−35 inhibited CYP2C8 activity in human and rat liver microsomes. EL−35 also decreased the expression of CYP2C8 in HepG2 cells. In the in vivo study, Tween 80 did not alter the PK of PTX after single or multiple doses, whereas EL−35 administered for 14 days significantly increased the AUC and MRT of PTX. Further analysis indicated that multiple-dose EL−35 reduced the expression of Cyp2c22 and production of 6-OH-PTX in the rat liver. Our study suggested that short-term exposure to both PEs did not affect the PK of PTX in rats, but multiple doses of EL−35 increased the AUC and MRT of PTX by downregulating the hepatic expression of Cyp2c22. Such effects should be taken into consideration during drug formulation and administration.

show abstract

Oral pharmacokinetic interaction of ester rich fruit juices and pharmaceutical excipients with tenofovir disoproxil fumarate in male Wistar rats

Cited by 6 publications

References 37 publications

Factors Contributing to the Antiviral Effectiveness of Tenofovir

Factors Contributing to the Antiviral Effectiveness of Tenofovir

Phytotherapy and Liver Disease

Assessing CYP2C8-Mediated Pharmaceutical Excipient-Drug Interaction Potential: A Case Study of Tween 80 and Cremophor EL−35

Contact Info

Product

Resources

About