An in vitro approach to study the absorption of a new oral formulation of berberine

Marino, Mirko; Gardana, Claudio; Scialpi, Antonio; Giorgini, Giuseppe; Simonetti, Paolo; Bò, Cristian Del

doi:10.1016/j.phanu.2021.100279

Cited by 4 publications

(4 citation statements)

References 41 publications

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“…We assume the electromotive force to be important for activity as the compounds had low passive permeability. A flip-flop mechanism has been suggested for triphenylphosphonium cations with a dependence on the voltage difference ( 37 ).…”

Section: Discussionmentioning

confidence: 99%

Delocalized quinolinium-macrocyclic peptides, an atypical chemotype for CNS penetration

Pingitore,

Pancholi,

Hornsby

et al. 2024

Sci. Adv.

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Macrocyclic drugs can address an increasing range of molecular targets but enabling central nervous system (CNS) access to these drugs has been viewed as an intractable problem. We designed and synthesized a series of quinolinium-modified cyclosporine derivatives targeted to the mitochondrial cyclophilin D protein. Modification of the cation to enable greater delocalization was confirmed by x-ray crystallography of the cations. Critically, greater delocalization improved brain concentrations. Assessment of the compounds in preclinical assays and for pharmacokinetics identified a molecule JP1-138 with at least 20 times the brain levels of a non-delocalized compound or those reported for cyclosporine. Levels were maintained over 24 hours together with low hERG potential. The paradigm outlined here could have widespread utility in the treatment of CNS diseases.

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Section: Discussionmentioning

confidence: 99%

Delocalized quinolinium-macrocyclic peptides, an atypical chemotype for CNS penetration

Pingitore,

Pancholi,

Hornsby

et al. 2024

Sci. Adv.

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“…The assessment of the intestinal permeability was performed through the evaluation of the transepithelial electrical resistance (TEER) and the transport of fluorescein isothiocyanatedextran (FITC-dextran). 36,37 Caco-2 cells with 80% confluence grade were seeded on Transwell® 24-well permeable media (12 mm, 0.4 μm pore polyester membranes) at a density of approximately 20 000 cells per well. Blank wells without cells were also included in the plate.…”

Section: Assessment Of Intestinal Permeability By Teer and Fitc Assaymentioning

confidence: 99%

Wild blueberry (V. angustifolium) improves TNFα-induced cell barrier permeability through claudin-1 and oxidative stress modulation in Caco-2 cells

Marino,

Venturi,

Rendine

et al. 2023

Food Funct.

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“…In an in vitro experiment on human colon adenocarcinoma cells (Caco-2) transwell model, developing a new formulation of berberine (nanoemulsion) revealed a notable improvement in the drug absorption (4.5 times at 25 C and 6 times at 80 C) as compared to the traditional formulation of the drug (Marino et al, 2021).…”

Section: "Bioavailability and Anti-diabetic Effectsmentioning

confidence: 99%

Pharmacokinetic of berberine, the main constituent of Berberis vulgaris L.: A comprehensive review

Khoshandam

Imenshahidi

Rahbardar

2022

Phytotherapy Research

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Barberry (Berberis vulgaris L.) is a medicinal plant and its main constituent is an isoquinoline alkaloid named berberine that has multiple pharmacological effects such as antioxidant, anti-microbial, antiinflammatory, anticancer, anti-diabetes, anti-dyslipidemia, and anti-obesity. However, it has restricted clinical uses due to its very poor solubility and bioavailability (less than 1%). It undergoes demethylenation, reduction, and cleavage of the dioxymethylene group in the first phase of metabolism. Its phase two reactions include glucuronidation, sulfation, and methylation. The liver is the main site for berberine distribution. Berberine could excrete in feces, urine, and bile.Fecal excretion of berberine (11-23%) is higher than urinary and biliary excretion routes. However, a major berberine metabolite is excreted in urine greater than in feces. Concomitant administration of berberine with other drugs such as metformin, cyclosporine A, digoxin, etc. may result in important interactions. Thus, in this review, we gathered and dissected any related animal and human research articles regarding the pharmacokinetic parameters of berberine including bioavailability, metabolism, distribution, excretion, and drug-drug interactions. Also, we discussed and gathered various animal and human studies regarding the developed products of berberine with better bioavailability and consequently, better therapeutic effects.

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An in vitro approach to study the absorption of a new oral formulation of berberine

Cited by 4 publications

References 41 publications

Delocalized quinolinium-macrocyclic peptides, an atypical chemotype for CNS penetration

Delocalized quinolinium-macrocyclic peptides, an atypical chemotype for CNS penetration

Wild blueberry (V. angustifolium) improves TNFα-induced cell barrier permeability through claudin-1 and oxidative stress modulation in Caco-2 cells

Pharmacokinetic of berberine, the main constituent of Berberis vulgaris L.: A comprehensive review

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