Skip to Main Content
+1 (508) 881-6771
0
Menu Button

Drug absorption

949

In vitro models replicating the human intestinal epithelium for absorption and metabolism studies: A systematic review

Absorption, distribution, metabolism and excretion (ADME) studies represent a fundamental step in the early stages of drug discovery. In particular, the absorption of orally administered drugs, which occurs at the intestinal level, has gained attention since poor oral bioavailability often led to failures for new drug approval. In this context, several in vitro preclinical models […]
921

In vitro reconstructed 3D corneal tissue models for ocular toxicology and ophthalmic drug development

Testing of all manufactured products and their ingredients for eye irritation is a regulatory requirement. In the last two decades, the development of alternatives to the in vivo Draize eye irritation test method has substantially advanced due to the improvements in primary cell isolation, cell culture techniques, and media, which have led to improved in […]
914

Bypassing P-glycoprotein mediated efflux of afatinib by cyclodextrin complexation – Evaluation of intestinal absorption and anti-cancer activity

A cyclodextrin complex of afatinib, a FDA-approved pan–ErbB inhibitor and known P-gp substrate, was developed to enhance its bio-activity while also reducing p-glycoprotein (P-gp) efflux, thereby improving its transport across the intestinal membrane. A sulfobutyl ether derivative of β-cyclodextrin (SBE-β-CD, pharmaceutical grade) was selected based on preliminary phase solubility studies and molecular modeling to prepare […]
886

In-Depth Characterization of EpiIntestinal Microtissue as a Model for Intestinal Drug Absorption and Metabolism in Human

The Caco-2 model is a well-accepted in vitro model for the estimation of fraction absorbed in human intestine. Due to the lack of cytochrome P450 3A4 (CYP3A4) activities, Caco-2 model is not suitable for the investigation of intestinal first-pass metabolism. The purpose of this study is to evaluate a new human intestine model, EpiIntestinal microtissues, […]
854

Nintedanib-Cyclodextrin Complex to Improve Bio-Activity and Intestinal Permeability

Cyclodextrin complex of nintedanib was prepared aiming for increased bio-activity and improved transport across intestinal membrane with reduced p-glycoprotein (p-gp) efflux. Based on preliminary phase solubility studies and molecular modeling, sulfobutyl ether derivative of β-cyclodextrin (SBE-β-CD, Captisol®) was selected to prepare inclusion complex. Complexation was confirmed using FTIR, 1H NMR, DSC, and XRD. Bioactivity of […]
839

Human 3D Gastrointestinal Microtissue Barrier Function As a Predictor of Drug-Induced Diarrhea

Drug-induced gastrointestinal toxicities (GITs) rank among the most common clinical side effects. Preclinical efforts to reduce incidence are limited by inadequate predictivity of in vitro assays. Recent breakthroughs in in vitro culture methods support intestinal stem cell maintenance and continual differentiation into the epithelial cell types resident in the intestine. These diverse cells self-assemble into microtissues with in […]
833

Human Primary Cell-Based Organotypic Microtissues for Modeling Small Intestinal Drug Absorption

Purpose: The study evaluates the use of new in vitro primary human cell-based organotypic small intestinal (SMI) microtissues for predicting intestinal drug absorption and drug-drug interaction. Methods: The microtissues were reconstructed using human intestinal fibroblasts and enterocytes cultured on a permeable support. To evaluate the suitability of the intestinal microtissues to model drug absorption, the permeability coefficients across the microtissues were determined for […]
815

In Vitro Skin Models and Their Predictability in Defining Normal and Disease Biology, Pharmacology, and Toxicity

In vitro skin model systems are increasingly being used both in the early evaluation of therapeutic drug candidates and in confirmatory mechanistic studies. The most commonly used of these in vitro model systems are reconstituted human epidermis (RHE) models. These RHE skin models consist solely of epidermal keratinocytes, which comes with some limitations but also with the advantage […]
798

A four-organ-chip for interconnected long-term co-culture of human intestine, liver, skin and kidney equivalents

Systemic absorption and metabolism of drugs in the small intestine, metabolism by the liver as well as excretion by the kidney are key determinants of efficacy and safety for therapeutic candidates. However, these systemic responses of applied substances lack in most in vitro assays. In this study, a microphysiological system maintaining the functionality of four organs over 28 […]
750

RECONSTRUCTION OF NEW ORGANOTYPIC 3D HUMAN SMALL INTESTINE TISSUE MODEL FOR DRUG SAFETY AND TOXICITY.

The epithelial lining of the gastrointestinal (GI) tract is a gatekeeper for entry of orally ingested nutrients and xenobiotics including medicaments. The small intestine has a well organized structure containing proliferative cells which migrate along the crypt-villi axis and differentiate into functionally mature epithelial cells. Currently, the most common in vitro model utilized for study […]
499

LINKER-BASED LECITHIN MICROEMULSIONS FOR TRANSDERMAL DELIVERY OF LIDOCAINE.

This study by researchers at the University of Toronto demonstrated that Mattek’s EpiDerm in vitro human skin tissue equivalent is an excellent in vitro alternative for examining the transdermal permeation and cytotoxicity characteristics of novel microemulsions. In this work, researchers at the University of Toronto introduce alcohol-free lecithin microemulsions formulated with linkers to produce transdermal […]
487

IN VITRO SKIN ABSORPTION AND DRUG RELEASE – A COMPARISON OF SIX COMMERCIAL PREDNICARBATE PREPARATIONS FOR TOPICAL USE.

This study by researchers at the Freie Universitat Berlin and Charite–Universitatsmedizin Berlin demonstrated that Mattek’s EpiDerm in vitro human skin tissue equivalent is an excellent in vitro model to study the potential skin metabolism of drugs designed to be applied to and/or penetrate human skin. Reconstructed human epidermis is a useful tool for in vitro […]