Active drug targeting: lessons learned and new things to consider.

Area of Science:

• Biomedical Engineering
• Nanotechnology
• Pharmacology

Background:

• Significant interest exists in passive and active drug targeting for in vivo diseased tissue treatment.
• Passive targeting commonly employs the enhanced permeation and retention (EPR) phenomenon for solid tumors and inflamed tissues.
• Active targeting involves conjugating targeting moieties (ligands) to delivery systems to bind upregulated receptors on diseased cells.

Purpose of the Study:

• To review the principles and applications of passive and active drug targeting strategies.
• To highlight the critical need for standardization in evaluating the efficiency of targeted drug delivery systems.
• To discuss the implications of assay heterogeneity on the future of active drug targeting research.

Main Methods:

• Review of existing literature on passive and active drug targeting mechanisms.
• Analysis of in vitro and in vivo assay methodologies for assessing targeting efficiency.
• Discussion on the impact of target validation and assay standardization.

Main Results:

• Passive targeting via EPR is a prevalent strategy for solid tumors and inflammation.
• Active targeting offers specificity through ligand-receptor interactions.
• Current methods for assessing targeting efficiency show significant heterogeneity.

Conclusions:

• Targeted drug delivery holds promise for various diseases, notably cancer.
• Standardization of in vitro and in vivo assays is paramount for accurate evaluation of targeting systems.
• Addressing assay heterogeneity is essential to prevent biased conclusions and advance active drug targeting.