In Vitro Permeability of Saponins and Sapogenins from Seed Extracts by the Parallel Artificial Membrane Permeability Assay: Effect of in Vitro Gastrointestinal Digestion

2020 ◽  
Vol 68 (5) ◽  
pp. 1297-1305 ◽  
Author(s):  
Joaquin Navarro del Hierro ◽  
Vieri Piazzini ◽  
Guillermo Reglero ◽  
Diana Martin ◽  
Maria Camilla Bergonzi
Keyword(s):  
Membrane Permeability ◽  
Artificial Membrane ◽  
Gastrointestinal Digestion ◽  
In Vitro Gastrointestinal Digestion ◽  
Permeability Assay ◽  
Seed Extracts

scholarly journals Paraben Transport and Metabolism in the Biomimetic Artificial Membrane Permeability Assay (BAMPA) and 3-Day and 21-Day Caco-2 Cell Systems

2006 ◽  
Vol 12 (1) ◽  
pp. 84-91 ◽  
Author(s):  
Mark Lakeram ◽  
David J. Lockley ◽  
David J. Sanders ◽  
Ruth Pendlington ◽  
Ben Forbes
Keyword(s):  
Membrane Permeability ◽  
Systemic Exposure ◽  
In Vitro Models ◽  
Log P ◽  
Hydroxybenzoic Acid ◽  
Artificial Membrane ◽  
Parabolic Relationship ◽  
Permeability Assay

Noncellular and cellular in vitro models for predicting intestinal absorption were used to investigate the transport and metabolism of parabens. The biomimetic artificial membrane permeability assay (BAMPA) membrane was constructed by impregnating a lipid solution on a hydrophobic filter. Caco-2 cells at passage numbers 65 to 80 were cultured in either the accelerated 3-day Biocoat™ system or the standard 21-day Transwell™ cell culture system. Paraben transport across the BAMPA system showed a parabolic relationship. The lowest log P (p-hydroxybenzoic acid) and highest log P compounds (heptyl and octyl parabens) had apparent permeabilities (Papp) less than 1.0 × 10-6 cm/s and Papp was maximal at approximately 8.5 × 10-6cm/s for the intermediate log P (ethylparaben) compound. With the Biocoat™, a similar parabolic relationship was found. In the 21-day Caco-2 cells, the parabens were metabolized by esterases at to p-hydroxybenzoic acid. In conclusion, the in vitro models added complementary insight into the absorption process, such as the transport route, intrinsic permeability, and extent of metabolism of the parabens. This study indicated that presystemic metabolism of orally ingested parabens to the p-hydroxybenzoic acid in the intestine may limit systemic exposure to alkyl-paraben esters in vivo.

scholarly journals Prediction of Permeation and Cellular Transport of Silybum marianum Extract Formulated in a Nanoemulsion by Using PAMPA and Caco-2 Cell Models

Planta Medica ◽  
2017 ◽  
Vol 83 (14/15) ◽  
pp. 1184-1193 ◽  
Author(s):  
Vieri Piazzini ◽  
Chiara Rosseti ◽  
Elisabetta Bigagli ◽  
Cristina Luceri ◽  
Anna Bilia ◽  
...  
Keyword(s):  
Membrane Permeability ◽  
Oral Delivery ◽  
Oral Absorption ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Cellular Transport ◽  
Artificial Membrane ◽  
Silybum Marianum ◽  
Permeability Assay

AbstractThe present study explores the potential of nanoemulsion, a lipid drug delivery system, to improve solubility and oral absorption of Silybum marianum extract. The optimized formulation contained 40 mg/mL of commercial extract (4 % w/w) and it was composed of 2.5 g labrasol (20 %) as the oil phase, 1.5 g cremophor EL as the surfactant, and 1 g labrafil as the cosurfactant (mixture surfactant/cosurfactant, 20 %).The system was characterized by dynamic light scattering, transmission electron microscopy, and HPLC-DAD analyses in order to evaluate size, homogeneity, morphology, and encapsulation efficiency. Physical and chemical stabilities were assessed during 40 days at 4 °C and 3 months at 25 °C. Stability in simulated gastric fluid followed by simulated intestinal conditions was also considered. In vitro permeation studies were performed to determine the suitability of the prepared nanoemulsion for oral delivery. Different models such as the parallel artificial membrane permeability assay and Caco-2 cell lines were applied.The nanoemulsion showed a good solubilizing effect of the extract, with a pronounced action also on its permeability, in respect to a saturated aqueous solution. The Caco-2 test confirmed the parallel artificial membrane permeability assay results and they revealed the suitability of the prepared nanoemulsion for oral delivery.

Wild pink bayberry fruit: the effect of in vitro gastrointestinal digestion on phytochemical profiles, and antioxidant and antiproliferative activities

2021 ◽  
Author(s):  
Wen Xia ◽  
Yanyun Lin ◽  
Ersheng Gong ◽  
Tong Li ◽  
Fengli Lian ◽  
...  
Keyword(s):  
Dietary Supplement ◽  
Antiproliferative Activity ◽  
Gastrointestinal Digestion ◽  
In Vitro Gastrointestinal Digestion ◽  
Phytochemical Profiles ◽  
Antiproliferative Activities

In general, pink bayberry cultivar, a vital source of polyphenols, showed strong antiproliferative activity after digestion at the end of the intestinal and colon steps, which can be considered as a dietary supplement.

scholarly journals Study on the chemical behaviour of bisphenol S during the in vitro gastrointestinal digestion and its bioaccessibility

2021 ◽  
pp. 130758
Author(s):  
Antía Lestido Cardama ◽  
Beatriz Millán Sánchez ◽  
Raquel Sendón ◽  
Ana Rodríguez Bernaldo de Quirós ◽  
Letricia Barbosa-Pereira
Keyword(s):  
Gastrointestinal Digestion ◽  
Bisphenol S ◽  
In Vitro Gastrointestinal Digestion ◽  
Chemical Behaviour

scholarly journals Characterization, Stability, and Bioaccessibility of Betalain and Phenolic Compounds from Opuntia stricta var. Dillenii Fruits and Products of Their Industrialization

Foods ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1593
Author(s):  
Iván Gómez-López ◽  
Gloria Lobo-Rodrigo ◽  
María P. Portillo ◽  
M. Pilar Cano
Keyword(s):  
Phenolic Compounds ◽  
Phenolic Acids ◽  
Total Phenolic ◽  
Antioxidant Compounds ◽  
Gastrointestinal Digestion ◽  
Fruit Peel ◽  
Full Characterization ◽  
In Vitro Gastrointestinal Digestion ◽  
Quercetin Glycoside

The aim of the present study was the full characterization, quantification, and determination of the digestive stability and bioaccessibility of individual betalain and phenolic compounds of Opuntia stricta, var. Dillenii fresh fruits (peel, pulp, and whole fruit) and of the products of the industrialization to obtain jam (raw pressed juice (product used for jam formulation), by-product (bagasse), and frozen whole fruit (starting material for jam production)). Opuntia stricta var. Dillenii fruits and products profile showed 60 betalain and phenolic compounds that were identified and quantified by HPLC-DAD-ESI/MS and HPLC-DAD-MS/QTOF, being 25 phenolic acids (including isomers and derivatives), 12 flavonoids (including glycosides), 3 ellagic acids (including glycosides and derivative), and 20 betanins (including degradation compounds). In vitro gastrointestinal digestion was performed by INFOGEST® protocol. Fruit pulp showed the greater content of total betalains (444.77 mg/100 g f.w.), and jam only showed very low amounts of two betanin degradation compounds, Cyclo-dopa-5-O-β-glucoside (and its isomer) (0.63 mg/100 f.w.), and two Phyllocactin derivatives (1.04 mg/100 g f.w.). Meanwhile, fruit peel was the richer tissue in total phenolic acids (273.42 mg/100 g f.w.), mainly in piscidic acid content and total flavonoids (7.39 mg/100 g f.w.), isorhamnetin glucoxyl-rhamnosyl-pentoside (IG2) being the most abundant of these compounds. The stability of betalains and phenolic compounds during in vitro gastrointestinal digestion is reported in the present study. In Opuntia stricta var. Dillenii pulp (the edible fraction of the fresh fruit), the betanin bioaccessibility was only 22.9%, and the flavonoid bioaccessibility ranged from 53.7% to 30.6%, depending on the compound. In non-edible samples, such as peel sample (PE), the betanin bioaccessibility was 42.5% and the greater bioaccessibility in flavonoids was observed for quercetin glycoside (QG1) 53.7%, the fruit peel being the most interesting material to obtain antioxidant extracts, attending to its composition on antioxidant compounds and their bioaccessibilities.

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