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Updated: May 31, 2026

A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction
Published on: August 27, 2019
Kinetic and thermodynamic approaches to the drug targeting phenomena
Igor Meerovich1, Alexander Koshkaryev, Vladimir P Torchilin
1Department of Pharmaceutical Sciences, Center for Pharmaceutical Biotechnology and Nanomedicine, Northeastern University, Boston, MA 02115, USA.
Abstract:
The effectiveness of many promising drug candidates (e.g. anticancer agents) awaits the development of drug forms capable of delivery of their drug load specifically to particular sites of an organism or a cell. To make universal and efficient drug carriers, administered drug-loaded vehicles should be able to reach the pathologic zone, recognize and bind their targets at a therapeutic concentration before clearance from the organism. Numerous methods have been developed to couple drug vehicles with active targeting substances - including monoclonal antibodies and substrates or ligands for pathologic cell receptors. Other approaches have included the use of such factors as decreased pH and elevated activity of enzymes in tumor tissues and the hypoxic environment inside the tumor core. This review makes an attempt to analyze the main factors that influence targeting on the kinetic or thermodynamic level that may provide the basis for a strategy to develop and improve drug delivery systems.
Insights
Developing effective drug delivery systems requires carriers that reach specific sites, bind targets, and maintain therapeutic concentrations. This review analyzes targeting factors to improve drug delivery strategies for enhanced treatment efficacy.
Area of Science:
- Biomedical Engineering
- Pharmacology
- Nanotechnology
Background:
- Effective drug delivery is crucial for many therapies, especially anticancer agents, but requires specialized drug carriers.
- Current drug carriers must reach target sites, bind effectively, and maintain therapeutic levels before organism clearance.
- Existing targeting strategies involve active targeting substances (e.g., antibodies) and exploiting tumor microenvironment characteristics (e.g., pH, hypoxia).
Purpose of the Study:
- To analyze the key factors influencing the targeting efficiency of drug delivery systems.
- To provide a basis for developing improved drug delivery strategies by examining kinetic and thermodynamic principles.
- To enhance the specificity and efficacy of drug carriers for therapeutic applications.
Main Methods:
- Review of existing literature on drug delivery systems and targeting mechanisms.
- Analysis of targeting strategies, including active targeting ligands and passive targeting based on tumor microenvironment.
- Examination of kinetic and thermodynamic principles governing drug-vehicle interactions and biodistribution.
Main Results:
- Targeting efficiency is influenced by factors such as ligand-receptor interactions, drug vehicle stability, and clearance rates.
- Tumor microenvironment characteristics (pH, hypoxia) offer passive targeting opportunities.
- Understanding kinetic and thermodynamic parameters is essential for optimizing drug delivery system design.
Conclusions:
- Improved drug delivery systems necessitate a comprehensive understanding of targeting mechanisms.
- Kinetic and thermodynamic analyses can guide the rational design of more effective drug carriers.
- Future strategies should focus on optimizing targeting to enhance therapeutic outcomes and minimize off-target effects.
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