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A Fluorescence-based Assay for Characterization and Quantification of Lipid Droplet Formation in Human Intestinal Organoids
Published on: October 13, 2019
Colloid formation by drugs in simulated intestinal fluid
Allison K Doak1, Holger Wille, Stanley B Prusiner
1Department of Pharmaceutical Chemistry, University of California-San Francisco, San Francisco, California 94158-2550, USA.
Journal of Medicinal Chemistry
|April 30, 2010
Summary
Many organic molecules and drugs form colloidal aggregates, potentially causing false positives in screening and affecting drug absorption. This study found six drugs form aggregates in simulated intestinal fluid at gut concentrations, impacting their in vivo behavior.
Area of Science:
- Biochemistry
- Pharmacology
- Drug Discovery
Background:
- Organic molecules can form colloidal aggregates in aqueous solutions at micromolar concentrations.
- These aggregates are known to promiscuously inhibit soluble proteins, leading to false positives in high-throughput screening.
- There is existing speculation regarding the impact of drug colloidal aggregation on in vivo absorption and distribution.
Purpose of the Study:
- To investigate the aggregation potential of drugs in simulated intestinal fluid.
- To determine if drug aggregation occurs at concentrations relevant to in vivo conditions.
- To assess the potential impact of drug aggregation on pharmacokinetic properties.
Main Methods:
- Tested 33 Biopharmaceutics Classification System (BCS) class II and IV drugs for aggregation in biochemical buffers.
- Identified 22 drugs exhibiting aggregation behavior.
- Assessed colloid formation of these 22 drugs in simulated intestinal fluid (SIF).
Main Results:
- Twenty-two out of 33 tested drugs showed promiscuous aggregation in biochemical buffers.
- Six of these drugs formed colloids in simulated intestinal fluid.
- Colloid formation occurred at concentrations equal to or lower than those found in the human gut.
Conclusions:
- Drug colloidal aggregation is a significant factor to consider in drug development.
- Six tested drugs may experience altered absorption and distribution in vivo due to colloid formation.
- These findings highlight the need to evaluate drug aggregation under physiological conditions to predict in vivo behavior.
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