Oral Drug Absorption

Yang, Yongsheng; Zhao, Yang; Yu, Alex; Sun, Duxin; Yu, Lawrence X.

doi:10.1016/b978-0-12-802447-8.00012-1

Cited by 16 publications

(2 citation statements)

References 75 publications

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“…Next, 100 µL aliquots were taken from both the apical and basolateral compartments, 300 µL of acetonitrile containing an internal standard was introduced, and the mixture was centrifuged for 10 min at 10,500× g, 4 • C. The supernatant was transferred to a vial and analyzed by liquid chro-matography coupled with tandem MS (LC-MS/MS). The AB (or BA) apparent permeability coefficients (P app , 10 -6 cm/s) were calculated according to the following formula [40,41]: P app = (V × ∆C)/(∆t × A × C 0 ), where V is the volume of the receiver compartment (cm 3 ), C 0 is the initial drug concentration in the donor compartment (µM), ∆C is the concentration in the receiver compartment (µM), ∆t is the incubation time (s), and A is the surface area of the cell monolayer (cm 2 ). An efflux ratio was calculated by dividing P app (BA) by P app (AB).…”

Section: Caco-2 Cell Penetrationmentioning

confidence: 99%

Naphthyl-Substituted Indole and Pyrrole Carboxylic Acids as Effective Antibiotic Potentiators—Inhibitors of Bacterial Cystathionine γ-Lyase

Kuzovlev,

Zybalov,

Golovin

et al. 2023

IJMS

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Over the past decades, the problem of bacterial resistance to most antibiotics has become a serious threat to patients’ survival. Nevertheless, antibiotics of a novel class have not been approved since the 1980s. The development of antibiotic potentiators is an appealing alternative to the challenging process of searching for new antimicrobials. Production of H2S—one of the leading defense mechanisms crucial for bacterial survival—can be influenced by the inhibition of relevant enzymes: bacterial cystathionine γ-lyase (bCSE), bacterial cystathionine β-synthase (bCBS), or 3-mercaptopyruvate sulfurtransferase (MST). The first one makes the main contribution to H2S generation. Herein, we present data on the synthesis, in silico analyses, and enzymatic and microbiological assays of novel bCSE inhibitors. Combined molecular docking and molecular dynamics analyses revealed a novel binding mode of these ligands to bCSE. Lead compound 2a manifested strong potentiating activity when applied in combination with some commonly used antibiotics against multidrug-resistant Acinetobacter baumannii, Pseudomonas aeruginosa, and methicillin-resistant Staphylococcus aureus. The compound was found to have favorable in vitro absorption, distribution, metabolism, excretion, and toxicity parameters. The high effectiveness and safety of compound 2a makes it a promising candidate for enhancing the activity of antibiotics against high-priority pathogens.

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Section: Caco-2 Cell Penetrationmentioning

confidence: 99%

Naphthyl-Substituted Indole and Pyrrole Carboxylic Acids as Effective Antibiotic Potentiators—Inhibitors of Bacterial Cystathionine γ-Lyase

Kuzovlev,

Zybalov,

Golovin

et al. 2023

IJMS

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“…Absorption is described as the path of the bioactive compound from the point of administration to the site of action [29,30]. The absorption of polyphenol is influenced by the physicochemical properties of the polyphenol.…”

Section: Biotransformation Of Polyphenols and Physiological Responsesmentioning

confidence: 99%

The Role of Genistein in Mammalian Reproduction

Guelfi,

Pasquariello,

Anipchenko

et al. 2023

Molecules

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Genistein is a natural compound belonging to flavonoids, having antioxidant, anti-inflammatory, and anti-neoplastic properties. Genistein is considered a phytoestrogen. As such, genistein can bind estrogen receptors (ERα and ERβ), although with a lower affinity than that of estradiol. Despite considerable work, the effects of genistein are not well established yet. This review aims to clarify the role of genistein on female and male reproductive functions in mammals. In females, at a high dose, genistein diminishes the ovarian activity regulating several pathway molecules, such as topoisomerase isoform I and II, protein tyrosine kinases (v-src, Mek-4, ABL, PKC, Syk, EGFR, FGFR), ABC, CFTR, Glut1, Glut4, 5α-reductase, PPAR-γ, mitogen-activated protein kinase A, protein histidine kinase, and recently circulating RNA-miRNA. The effect of genistein on pregnancy is still controversial. In males, genistein exerts an estrogenic effect by inducing testosterone biosynthesis. The interaction of genistein with both natural and synthetic endocrine disruptors has a negative effect on testis function. The positive effect of genistein on sperm quality is still in debate. In conclusion, genistein has a potentially beneficial effect on the mechanisms regulating the reproduction of females and males. However, this is dependent on the dose, the species, the route, and the time of administration.

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Lateral Assessment of Mucomimetic Hydrogels to Evaluate Correlation between Microscopic and Macroscopic Properties

Faurschou,

Clasky,

Watchorn

et al. 2024

Macromolecular Bioscience

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A major limitation in the development of mucosal drug delivery systems is the design of in vitro models that accurately reflect in vivo conditions. Traditionally, models seek to mimic characteristics of physiological mucus, often focusing on property‐specific trial metrics such as rheological behavior or diffusion of a nanoparticle of interest. Despite the success of these models, translation from in vitro results to in vivo trials is limited. As a result, several authors have called for work to develop standardized testing methodologies and characterize the influence of model properties on drug delivery performance. To this end, a series of trials is performed on 12 mucomimetic hydrogels reproduced from literature. Experiments show that there is no consistent correlation between barrier performance and rheological or microstructural properties of the tested mucomimetic hydrogels. In addition, the permeability of both mucopenetrating and mucoadhesive nanoparticles is assessed, revealing non‐obvious variations in barrier properties such as the relative contributions of electrostatic and hydrophobic interactions in different models. These results demonstrate the limitations of predicting mucomimetic behavior with common characterization techniques and highlight the importance of testing barrier performance with multiple nanoparticle formulations.

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Oral Drug Absorption

Cited by 16 publications

References 75 publications

Naphthyl-Substituted Indole and Pyrrole Carboxylic Acids as Effective Antibiotic Potentiators—Inhibitors of Bacterial Cystathionine γ-Lyase

Naphthyl-Substituted Indole and Pyrrole Carboxylic Acids as Effective Antibiotic Potentiators—Inhibitors of Bacterial Cystathionine γ-Lyase

The Role of Genistein in Mammalian Reproduction

Lateral Assessment of Mucomimetic Hydrogels to Evaluate Correlation between Microscopic and Macroscopic Properties

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