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Methods for Studying Drug Absorption: In vitro

Methods for Studying Drug Absorption: In vitro

In vitro experiments are crucial for understanding the transport and absorption of drugs through biological materials. These studies employ varied methods such as the diffusion cell method, the everted sac technique, and the everted ring technique.
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...

Renewal of Intestinal Stem Cells

Renewal of Intestinal Stem Cells

The intestinal epithelial lining rapidly renews every 4 to 5 days. The renewal is facilitated by intestinal stem cells (ISCs) located at the base of the crypt– a gland located at the bottom of each villus. ISCs divide asymmetrically to form new stem cells and progenitor daughter cells. The daughter cells are called transit-amplifying (TA) cells which move upwards along the crypt and either differentiate into absorptive cells– the enterocytes or secretory cells– including the goblet,...

Carbohydrate Absorption

Carbohydrate Absorption

Carbohydrates are essential macronutrients that serve as the body's primary energy source. Their digestion begins in the mouth, where salivary amylase partially breaks down complex carbohydrates such as starch into smaller oligosaccharides. This mechanical and enzymatic activity prepares carbohydrates for further processing in the gastrointestinal tract.
After being swallowed, the partially digested carbohydrates mix with gastric secretions in the stomach. However, the acidic environment...

Absorption of Nutrients

Absorption of Nutrients

Absorption refers to taking dietary nutrients from the intestinal lumen for transportation throughout the body. After digestion in the small intestine, carbohydrates, proteins, and fats are broken down into simpler forms. These essential macronutrients and other vital substances, such as vitamins, minerals, and water, are then prepared for absorption into the bloodstream.
Enterocytes, which are specialized polar epithelial cells, line the mucosa of the small intestinal walls. These cells...

Glucose Absorption Into the Small Intestine

Glucose Absorption Into the Small Intestine

Complex carbohydrates consumed cannot be absorbed into the small intestine in their original form. First, they must be hydrolyzed to a monosaccharide form such as glucose or galactose. These monosaccharides are then transported across the intestinal membrane and into the blood via transcellular transport. The intestinal epithelial cells allow the movement of these monosaccharides with a defined 'entry' through membrane transporter proteins present on their apical membrane and 'exit' via the...

Histology of the Small Intestine

Histology of the Small Intestine

The small intestine exhibits a unique histological structure that significantly enhances its function in digestion and nutrient absorption. These structures include circular folds, villi, and various specialized cells that collectively facilitate the digestion of food.
The intestinal lining features transverse folds called circular folds, each housing fingerlike projections known as intestinal villi. These villi are covered by a layer of simple columnar epithelium, also referred to as...

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Related Experiment Video

Updated: Jun 3, 2026

Using Caco-2 Cells to Study Lipid Transport by the Intestine

Using Caco-2 Cells to Study Lipid Transport by the Intestine

Published on: August 20, 2015

Caco-2 cells as a model for intestinal absorption.

Isabella De Angelis¹, Laura Turco

¹Istituto Superiore di Sanità, Rome, Italy.

Current Protocols in Toxicology

|March 15, 2011

Summary

This summary is machine-generated.

The Caco-2 cell system effectively predicts oral drug absorption in humans by assessing intestinal barrier permeability. Careful standardization and calibration are key for reliable results in drug discovery.

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The Caco-2 Cell Bioassay for Measurement of Food Iron Bioavailability

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Using Caco-2 Cells to Study Lipid Transport by the Intestine

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The Caco-2 Cell Bioassay for Measurement of Food Iron Bioavailability

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Published on: April 28, 2022

Area of Science:

Pharmacology
Cell Biology
Drug Discovery

Background:

The Caco-2 cell system is a validated in vitro model for studying intestinal absorption.
It allows for the evaluation of chemical compound permeability across the intestinal barrier.
This model is increasingly used to understand drug transport mechanisms.

Purpose of the Study:

To highlight the utility of the Caco-2 cell system in predicting oral absorption.
To emphasize its role as a screening tool in drug discovery for intestinal permeability.
To discuss the importance of experimental standardization for in vivo correlation.

Main Methods:

Utilizing the Caco-2 cell line as an intestinal in vitro model.
Measuring chemical and drug permeability across the Caco-2 cell monolayer.
Correlating in vitro permeability data with human in vivo absorption data.

Main Results:

Permeability values from the Caco-2 model show good correlation with human in vivo absorption data for many substances.
The Caco-2 system is a valuable tool for predicting intestinal drug permeability.
Its application is expanding within drug discovery strategies.

Conclusions:

The Caco-2 cell system is a reliable model for predicting oral absorption and intestinal drug permeability.
Strict adherence to experimental conditions and cell culture protocols is essential for accurate predictions.
Calibration with internal reference compounds is crucial for inter-laboratory data comparability and validation.