Rapid in vitro test to predict ocular tissue permeability based on biopartitioning micellar chromatography

Martı́n-Biosca, Yolanda; Molero-Monfort, M.; Sagrado, S.; Villanueva-Camañas, R.M.; Medina-Hernández, M.J.

doi:10.1016/s0928-0987(03)00195-7

Cited by 22 publications

(6 citation statements)

References 10 publications

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“…At the same time, these parts constitute a main route for ophthalmic drugs. The consequence of such duality is a debate regarding the permeability of the eye [1,2,3,4,5].…”

Section: Introductionmentioning

confidence: 99%

Targeted Drug Delivery Systems for the Treatment of Glaucoma: Most Advanced Systems Review

Olga

2019

Polymers

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Each year, new glaucoma drug delivery systems are developed. Due to the chronic nature of the disease, it requires the inconvenient daily administration of medications. As a result of their elution from the eye surface and penetration to the bloodstream through undesired permeation routes, the bioavailability of active compounds is low, and systemic side effects occur. Despite numerous publications on glaucoma drug carriers of controlled drug release kinetics, only part of them consider drug permeation routes and, thus, carriers’ location, as an important factor affecting drug delivery. In this paper, we try to demonstrate the importance of the delivery proximal to glaucoma drug targets. The targeted delivery can significantly improve drug bioavailability, reduce side effects, and increase patients’ compliance compared to both commercial and scientifically developed formulations that can spread over the eye surface or stay in contact with conjunctival sac. We present a selection of glaucoma drug carriers intended to be placed on cornea or injected into the aqueous humor and that have been made by advanced materials using hi-tech forming methods, allowing for effective and convenient sustained antiglaucoma drug delivery.

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“…At the same time, these parts constitute a main route for ophthalmic drugs. The consequence of such duality is a debate regarding the permeability of the eye [1,2,3,4,5].…”

Section: Introductionmentioning

confidence: 99%

Targeted Drug Delivery Systems for the Treatment of Glaucoma: Most Advanced Systems Review

Olga

2019

Polymers

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“…MLC has been applied to a variety of applications including prediction of transdermal permeation (Waters, Shahzad, & Stephenson, ) through to oral drug absorption (Escuder‐Gilabert, Martınez‐Pla, Sagrado, Villanueva‐Camañas, & Medina‐Hernández, ), blood–brain barrier penetration (Escuder‐Gilabert, Molero‐Monfort, Villanueva‐Camañas, Sagrado, & Medina‐Hernández, ) and ocular tissue permeability (Martın‐Biosca, Molero‐Monfort, Sagrado, Villanueva‐Camañas, & Medina‐Hernández, ). In recent years, studies have also attempted to link chromatographically derived retention constants with pharmacokinetic predictors determined in silico , and although linear relationships have been found (Milošević, Stojanović, Penov‐Gaši, Perišić‐Janjić, & Kaliszan, ), these previously published studies depend upon the reliability of calculated data whereas this work attempts to correlate chromatographic data with published experimental data.…”

Section: Introductionmentioning

confidence: 99%

Prediction of human intestinal absorption using micellar liquid chromatography with an aminopropyl stationary phase

Shokry

Waters

Parkes

et al. 2019

Biomedical Chromatography

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The extent of human intestinal absorption (HIA) for a drug is considered to be an important pharmacokinetic parameter which must be determined for orally administered drugs. Traditional experimental methods relied upon animal testing and are renowned for being time consuming and expensive as well as being ethically unfavourable. As a result, the development of alternative methods to evaluate a drug's pharmacokinetics is crucial. Micellar liquid chromatography is considered to be one of these methods that can replace the use of animals in the prediction of HIA. In this study, the combination of an aminopropyl column with the biosurfactant sodium deoxycholate bile salt was used in the experimental determination of micelle–water partition coefficients (log Pmw) for a group of compounds. Multiple linear regression was then used for the prediction of HIA using the experimentally determined log Pmw along with other molecular descriptors, leading to the construction of a model equation of R2 = 85% and a prediction power represented by R2Pred. = 72%. The use of micellar liquid chromatography with an aminopropyl column in combination with sodium deoxycholate was found to be a good method for the prediction of human intestinal absorption, providing data for a far wider range of compounds compared with previous studies.

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“…The MELC, which utilizes microemulsions as a mobile phase and has been shown to be suitable for the separation of a range of pharmaceutical compounds using both isocratic and gradient elution modes 18 and for validated determinations of fosinoprilat in human plasma and simvastatin and its impurities in bulk drug and tablet formulations 19. Also biopartitioning micellar chromatography (BMC) has been used in modelling many biopartitioning processes, including human drug absorption,20 BBB penetration,21 ocular tissue permeability,22 skin permeability,23 etc. Using a microemulsion as the mobile phase alters the solutes partitioning between the mobile and stationary phase characteristics in comparison with conventional HPLC because a layer of surfactant molecules adsorbs on the surface of the stationary phase.…”

Section: Introductionmentioning

confidence: 99%

Prediction of polar surface area of drug molecules: A QSPR approach

Noorizadeh

Farmany

Noorizadeh

et al. 2011

Drug Testing and Analysis

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A quantitative structure-property relationship (QSPR) study based on an artificial neural network (ANN) was carried out for the prediction of the microemulsion liquid chromatography polar surface area (PSA) of a set of 32 drug compounds. The genetic algorithm-kernel partial least squares (GA-KPLS) method was used as a variable selection tool. A KPLS method was used to select the best descriptors and the selected descriptors were used as input neurons in neural network model. For choosing the best predictive model from among comparable models, square correlation coefficient Q(2) for the whole set calculated based on leave-group-out predicted values of the training set and model-derived predicted values for the test set compounds is suggested to be a good criterion. Finally, to improve the results, structure-property relationships were followed by nonlinear approach using artificial neural networks and consequently better results were obtained. Also this demonstrates the advantages of ANN.

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Rapid in vitro test to predict ocular tissue permeability based on biopartitioning micellar chromatography

Cited by 22 publications

References 10 publications

Targeted Drug Delivery Systems for the Treatment of Glaucoma: Most Advanced Systems Review

Targeted Drug Delivery Systems for the Treatment of Glaucoma: Most Advanced Systems Review

Prediction of human intestinal absorption using micellar liquid chromatography with an aminopropyl stationary phase

Prediction of polar surface area of drug molecules: A QSPR approach

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