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Active targeting with particulate drug carriers in tumor therapy: fundamentals and recent progress
Fabrizio Marcucci1, François Lefoulon
1Reparto di Epidemiologia Clinica, Istituto Superiore di Sanità, Viale Regina Elena 299, 00161 Rome, Italy.
Abstract:
Drug therapy for the treatment of tumors is often limited by a narrow therapeutic index. One approach that overcomes this limitation is the active targeting of tumors with particulate drug carriers. The derivatization of particulate drug carriers with a ligand leads to the selective targeting of the particulate to selected cells, thereby focusing drug delivery. In addition, particulate drug carriers have a high loading capacity, do not need covalent conjugation of the drug and the formulation protects the entrapped drug from enzymatic inactivation. Despite these favorable properties, their therapeutic efficacy in animal models has been reported only in recent years. The use of internalizing ligands and the targeting of intravascular tumor cells and endothelial cells of tumor blood vessels have been instrumental in demonstrating the clinical effectiveness of particulate drug carriers in animal models. As a result, several actively targeted particulate carriers have now entered, or are about to enter, clinical investigation. Recent findings, for example, the identification of cell-penetrating peptides with restricted cell selectivity, suggest that further improvements in this approach are likely in the near future.
Insights
Targeted drug delivery using particulate carriers improves tumor treatment by overcoming drug limitations. Recent advances in targeting strategies are enhancing their clinical effectiveness in animal models and human trials.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Pharmacology
Background:
- Drug therapy for tumors faces limitations due to narrow therapeutic indices.
- Particulate drug carriers offer a promising strategy to overcome these limitations through active targeting.
- These carriers possess high drug loading capacity and protect drugs from degradation.
Purpose of the Study:
- To review the advancements in actively targeted particulate drug carriers for tumor treatment.
- To highlight the key strategies and findings demonstrating their therapeutic efficacy.
- To discuss the future potential of improved targeting ligands.
Main Methods:
- Review of recent scientific literature on particulate drug carriers and tumor targeting.
- Analysis of studies demonstrating therapeutic efficacy in animal models.
- Examination of clinical trial progress for actively targeted carriers.
Main Results:
- Active targeting of tumors with particulate carriers, using ligands, enhances drug delivery specificity.
- Internalizing ligands and targeting tumor vasculature have been crucial for demonstrating efficacy in vivo.
- Several actively targeted particulate carriers are now in clinical investigation.
Conclusions:
- Actively targeted particulate drug carriers show significant promise for improved cancer therapy.
- Ongoing research into novel targeting ligands, like cell-penetrating peptides, is expected to further enhance efficacy.
- These advanced drug delivery systems are transitioning from preclinical to clinical applications.
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