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Updated: Mar 11, 2026
Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
Published on: October 17, 2013
Passive drug permeation through membranes and cellular distribution
1Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Inc., Cambridge, MA 02139, United States.
Passive drug distribution mechanisms, like lipoidal diffusion and pH partitioning, are crucial for intracellular drug action. Understanding these passive cellular permeation processes aids in designing safer, more effective therapeutics.
Area of Science:
- Pharmacology
- Cell Biology
- Drug Delivery
Background:
- Passive mechanisms significantly influence drug distribution within cells.
- Lipoidal diffusion and pH partitioning are key passive processes affecting intracellular drug accumulation.
- These mechanisms are vital for achieving targeted drug action at the intracellular level.
Purpose of the Study:
- To review passive mechanisms of cellular drug permeation.
- To highlight the exploitation of these mechanisms in drug design.
- To provide a mathematical model for understanding intracellular drug distribution.
Main Methods:
- Review of existing literature on passive drug permeation.
- Development of a generic mathematical model of cellular drug distribution.
- Discussion of methods for parameter estimation and measurement of intracellular drug concentrations.
Main Results:
- Passive mechanisms like lipoidal diffusion and pH partitioning are critical for intracellular drug accumulation.
- These processes are increasingly utilized in developing effective and safe drugs.
- A mathematical model illustrates steady-state intracellular drug distribution.
Conclusions:
- Passive cellular drug permeation mechanisms are essential for effective intracellular drug targeting.
- Understanding and modeling these processes can guide the design of novel therapeutics.
- Methods for quantifying intracellular drug concentrations are key to evaluating drug efficacy.
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