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Drug Distribution: Tissue Binding

Drug Distribution: Tissue Binding

Upon entering the systemic circulation, drugs can distribute into the interstitial and intracellular fluid of various tissue cells. This distribution is facilitated by the binding of drugs to different cellular components within tissues, which may lead to drug accumulation in specific areas. Drugs bound to tissue components serve as reservoirs that release free drugs back into the system, prolonging the drug's overall action. However, this accumulation can also result in local toxicity.
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Related Experiment Video

Updated: Oct 22, 2025

Spatial Quantification of Drugs in Pulmonary Tuberculosis Lesions by Laser Capture Microdissection Liquid Chromatography Mass Spectrometry LCM-LC/MS

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Visualizing and quantifying antimicrobial drug distribution in tissue.

Benjamin A Kuzma¹, Isaac J Pence¹, Daniel A Greenfield¹

¹Wellman Center for Photomedicine, Massachusetts General Hospital, Harvard Medical School, Boston 02114, USA.

Advanced Drug Delivery Reviews

|August 26, 2021

Summary

This summary is machine-generated.

Accurately measuring drug efficacy at the site of action is crucial. Image-guided approaches offer a non-invasive solution to quantify drug biodistribution and pharmacokinetics, improving our understanding of treatment effectiveness.

Keywords:

Antimicrobials Biodistribution CT Fluorescence MRI Mass spectrometry PET Pharmacokinetics Raman SPECT

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Published on: December 24, 2016

Area of Science:

Pharmacology
Biomedical Imaging
Drug Delivery

Background:

Accurate assessment of drug efficacy requires understanding drug concentration at the target site.
Current methods often use plasma drug concentration as a surrogate, which may not reflect actual tissue drug levels.
This discrepancy poses a challenge in mechanistic understanding and optimizing antimicrobial treatments.

Purpose of the Study:

To review and evaluate various imaging modalities for quantifying drug biodistribution and pharmacokinetics at the site of action.
To highlight the advantages of image-guided approaches over traditional surrogate measurements.
To discuss the progress, limitations, and future potential of different imaging techniques in drug research.

Main Methods:

Review of imaging modalities including radio-labeling, magnetic resonance imaging (MRI), mass spectrometry imaging (MSI), computed tomography (CT), fluorescence imaging, and Raman spectroscopy.
Examples provided range from in vitro cellular drug uptake studies to clinical applications in microbial infections.
Focus on image-guided quantification of drug distribution within specific tissues or sites of action.

Main Results:

Image-guided approaches enable accurate quantification of drug biodistribution and pharmacokinetics at the intended site of action.
Various imaging modalities show promise, each with unique strengths and limitations for visualizing drug distribution.
Non-invasive optical imaging techniques offer significant potential for deeper insights with reduced patient burden.

Conclusions:

Image-guided drug biodistribution and pharmacokinetic studies are essential for a mechanistic understanding of drug efficacy.
Advancements in non-invasive imaging modalities can provide more profound insights into drug action.
Improved imaging techniques will benefit both researchers and patients by offering more accurate and less burdensome measurement approaches.