PHOTORESPONSIVE ARTIFICIAL MEMBRANE. REGULATION OF MEMBRANE PERMEABILITY OF LIPOSOMAL MEMBRANE BY PHOTOREVERSIBLE CIS-TRANS ISOMERIZATION OF AZOBENZENES

1981 ◽  
Vol 34 (3) ◽  
pp. 323-329 ◽  
Author(s):  
Kaji Kano ◽  
Yasuhiko Tanaka ◽  
Teiichiro Ogawa ◽  
Masatsugu Shimomura ◽  
Toyoki Kunitake
Keyword(s):  
Membrane Permeability ◽  
Artificial Membrane ◽  
Liposomal Membrane ◽  
Trans Isomerization

scholarly journals Prediction of Parallel Artificial Membrane Permeability Assay of Some Drugs from their Theoretically Calculated Molecular Descriptors

2011 ◽  
Vol 8 (3) ◽  
pp. 1074-1085
Author(s):  
E. Konoz ◽  
Amir H. M. Sarrafi ◽  
S. Ardalani
Keyword(s):  
Neural Network ◽  
Membrane Permeability ◽  
Selection Procedure ◽  
Structure Property ◽  
Artificial Membrane ◽  
Structure Property Relationships ◽  
Quantitative Structure Property Relationships ◽  
Artificial Neural ◽  
Variable Subset Selection ◽  
Mlr Model

Parallel artificial membrane permeation assays (PAMPA) have been extensively utilized to determine the drug permeation potentials. In the present work, the permeation of miscellaneous drugs measured as flux by PAMPA (logF) of 94 drugs, are predicted by quantitative structure property relationships modeling based on a variety of calculated theoretical descriptors, which screened and selected by genetic algorithm (GA) variable subset selection procedure. These descriptors were used as inputs for generated artificial neural networks. After generation, optimization and training of artificial neural network (5:3:1), it was used for the prediction of logF for the training, test and validation sets. The standard error for the GA-ANN calculated logF for training, test and validation sets are 0.17, 0.028 and 0.15 respectively, which are smaller than those obtained by GA-MLR model (0.26, 0.051 and 0.22, respectively). Results obtained reveal the reliability and good predictably of neural network model in the prediction of membrane permeability of drugs.

Prediction of human intestinal permeability using artificial membrane permeability

2003 ◽  
Vol 257 (1-2) ◽  
pp. 245-251 ◽  
Author(s):  
Kiyohiko Sugano ◽  
Yoshiaki Nabuchi ◽  
Minoru Machida ◽  
Yoshinori Aso
Keyword(s):  
Membrane Permeability ◽  
Intestinal Permeability ◽  
Artificial Membrane

scholarly journals Flavonoids modulate liposomal membrane structure, regulate mitochondrial membrane permeability and prevent erythrocyte oxidative damage

2020 ◽  
Vol 1862 (11) ◽  
pp. 183442 ◽  
Author(s):  
Artem G. Veiko ◽  
Szymon Sekowski ◽  
Elena A. Lapshina ◽  
Agnieszka Z. Wilczewska ◽  
Karolina H. Markiewicz ◽  
...  
Keyword(s):  
Oxidative Damage ◽  
Membrane Permeability ◽  
Mitochondrial Membrane ◽  
Membrane Structure ◽  
Liposomal Membrane ◽  
Mitochondrial Membrane Permeability

Ion movements in membrane vesicles: a new fluorescence method and application to smooth muscle

1985 ◽  
Vol 248 (3) ◽  
pp. C372-C378 ◽  
Author(s):  
A. K. Grover ◽  
A. P. Singh ◽  
P. K. Rangachari ◽  
P. Nicholls
Keyword(s):  
Membrane Potential ◽  
Membrane Permeability ◽  
Membrane Vesicles ◽  
Liposomal Membrane ◽  
Phosphatidylcholine Liposomes ◽  
Permeability Characteristics ◽  
Cation Permeability ◽  
Ion Movements ◽  
Rate Of Dissipation ◽  
Very High

A method is described for studying ion permeabilities of membrane vesicles based on the principle that when membrane permeability to H+ is very high, the H+ movement is determined by the membrane potential generated by the H+ movement. The rate of H+ movement under these conditions thus gives a measure of the rate of dissipation of this membrane potential by comovement of anions or countermovement of cations present. Thus, by studying the H+ efflux using an impermeant cation and different anions, the membrane permeability to the anions can be assessed. Similarly, the use of an impermeant anion allows the study of the permeation of various cations. H+ movement was followed across the membranes by monitoring a change in the fluorescence intensity of the pH-sensitive dye pyranine trapped inside the membranes. This method when tested using phosphatidylcholine liposomes yielded the expected results, i.e., permeability of the liposomal membrane was: Cl- greater than SO2-4 and K+ greater than Na+. A plasma membrane-enriched fraction loaded with pyranine was isolated from estrogen-dominant rat myometrium. The anion permeability characteristics of this membrane were studied using tetramethylammonium (TMA+) as the poorly permeant cation, and the cation permeability was studied using L-glutamate- as the poorly permeant anion. The anion permeabilities were D-glutamate- less than L-glutamate- less than glutarate2- less than Cl- less than or equal to SO2-4, and the cation permeabilities were TMA+ less than K+ less than Na+. It is hypothesized that the observed anomalously higher Na+ and SO2-4 movements may involve special mechanisms.

scholarly journals Biomimetic Artificial Membrane Permeability Assay over Franz Cell Apparatus Using BCS Model Drugs

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 988
Author(s):  
Leonardo de Souza Teixeira ◽  
Tatiana Vila Chagas ◽  
Antonio Alonso ◽  
Isabel Gonzalez-Alvarez ◽  
Marival Bermejo ◽  
...  
Keyword(s):  
Membrane Permeability ◽  
Electron Paramagnetic Resonance Spectroscopy ◽  
Oral Drug ◽  
Resonance Spectroscopy ◽  
Artificial Membrane ◽  
Apparent Permeability ◽  
Franz Cell ◽  
Bcs Model ◽  
Fda Guidance ◽  
Permeability Assay

A major parameter controlling the extent and rate of oral drug absorption is permeability through the lipid bilayer of intestinal epithelial cells. Here, a biomimetic artificial membrane permeability assay (Franz–PAMPA Pampa) was validated using a Franz cells apparatus. Both high and low permeability drugs (metoprolol and mannitol, respectively) were used as external standards. Biomimetic properties of Franz–PAMPA were also characterized by electron paramagnetic resonance spectroscopy (EPR). Moreover, the permeation profile for eight Biopharmaceutic Classification System (BCS) model drugs cited in the FDA guidance and another six drugs (acyclovir, cimetidine, diclofenac, ibuprofen, piroxicam, and trimethoprim) were measured across Franz–PAMPA. Apparent permeability (Papp) Franz–PAMPA values were correlated with fraction of dose absorbed in humans (Fa%) from the literature. Papp in Caco-2 cells and Corti artificial membrane were likewise compared to Fa% to assess Franz–PAMPA performance. Mannitol and metoprolol Papp values across Franz–PAMPA were lower (3.20 × 10−7 and 1.61 × 10−5 cm/s, respectively) than those obtained across non-impregnated membrane (2.27 × 10−5 and 2.55 × 10−5 cm/s, respectively), confirming lipidic barrier resistivity. Performance of the Franz cell permeation apparatus using an artificial membrane showed acceptable log-linear correlation (R2 = 0.664) with Fa%, as seen for Papp in Caco-2 cells (R2 = 0.805). Data support the validation of the Franz–PAMPA method for use during the drug discovery process.

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.

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