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Updated: Mar 13, 2026

Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?
Published on: June 13, 2014
The achievement of ligand-functionalized organic/polymeric nanoparticles for treating multidrug resistant cancer
Wing-Hin Lee1, Ching-Yee Loo1, Chean-Ring Leong2
1a Respiratory Technology, Woolcock Institute of Medical Research and Discipline of Pharmacology, Sydney Medical School , University of Sydney , Sydney , Australia.
Introduction:
The effectiveness of conventional cancer chemotherapy is hampered by the occurrence of multidrug resistance (MDR) in tumor cells. Although many studies have reported the development of novel MDR chemotherapeutic agents, clinical success is lacking owing to the high associated toxicity. Nanoparticle-based delivery of chemotherapeutic drugs has emerged as alternative approach to treat MDR cancers via exploitation of leaky vasculature in the tumor microenvironment. Accordingly, functionalization of nanoparticles with target specific ligands can be employed to achieve significant improvements in the treatment of MDR cancer. Areas covered: This review focuses on the recent advances in the functionalization of nanocarriers with specific ligands, including antibodies, transferrin, folate, and peptides to overcome MDR cancer. The limitations of effective ligand-functionalized nanoparticles as well as therapeutic successes in ligand targeting are covered in the review. Expert opinion: Targeting MDR tumors with ligand-functionalized nanoparticles is a promising approach to improve the treatment of cancer. With this approach, higher drug concentrations at targeted sites would be achieved with lower dosage frequencies and reduced side effects in comparison to existing formulations of chemotherapeutic drugs. However, potential toxicities and immunological responses to ligands should be carefully reviewed for viable options in for future MDR cancer treatment.
Insights
Ligand-functionalized nanoparticles offer a promising strategy to overcome multidrug resistance (MDR) in cancer. This approach enhances drug delivery to tumors, potentially reducing side effects and improving treatment outcomes for MDR cancers.
Area of Science:
- Oncology
- Nanotechnology
- Drug Delivery
Background:
- Multidrug resistance (MDR) significantly limits the effectiveness of conventional cancer chemotherapy.
- High toxicity of novel MDR chemotherapeutic agents hinders clinical success.
- Nanoparticle-based drug delivery offers a promising alternative for treating MDR cancers by exploiting tumor microenvironment characteristics.
Purpose of the Study:
- To review recent advances in functionalizing nanocarriers with specific ligands to overcome MDR in cancer.
- To discuss the limitations and therapeutic successes of ligand-functionalized nanoparticles in targeting MDR tumors.
Main Methods:
- Focus on ligand functionalization of nanocarriers using antibodies, transferrin, folate, and peptides.
- Review of literature on nanoparticle targeting strategies for MDR cancer.
Main Results:
- Ligand-functionalized nanoparticles can improve drug delivery to MDR tumors.
- Targeting MDR tumors with these nanoparticles may lead to higher drug concentrations at the tumor site.
- This approach has the potential for lower dosage frequencies and reduced systemic side effects.
Conclusions:
- Targeting MDR tumors with ligand-functionalized nanoparticles is a promising strategy for improved cancer treatment.
- Potential toxicities and immunological responses associated with ligands require careful evaluation for future clinical applications.
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