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Updated: Jun 7, 2026

A Comprehensive Procedure to Evaluate the In Vivo Performance of Cancer Nanomedicines
Published on: March 4, 2017
Receptor-targeted nanocarriers for therapeutic delivery to cancer
Bo Yu1, Heng Chiat Tai, Weiming Xue
1Department of Chemical and Biomolecular Engineering, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, USA.
Abstract:
Efficient and site-specific delivery of therapeutic drugs is a critical challenge in clinical treatment of cancer. Nano-sized carriers such as liposomes, micelles, and polymeric nanoparticles have been investigated for improving bioavailability and pharmacokinetic properties of therapeutics via various mechanisms, for example, the enhanced permeability and retention (EPR) effect. Further improvement can potentially be achieved by conjugation of targeting ligands onto nanocarriers to achieve selective delivery to the tumour cell or the tumour vasculature. Indeed, receptor-targeted nanocarrier delivery has been shown to improve therapeutic responses both in vitro and in vivo. A variety of ligands have been investigated including folate, transferrin, antibodies, peptides and aptamers. Multiple functionalities can be incorporated into the design of nanoparticles, e.g., to enable imaging and triggered intracellular drug release. In this review, we mainly focus on recent advances on the development of targeted nanocarriers and will introduce novel concepts such as multi-targeting and multi-functional nanoparticles.
Insights
Targeted nanocarriers improve cancer drug delivery by selectively targeting tumor cells. Advanced designs incorporate multi-targeting and multi-functional nanoparticles for enhanced therapeutic efficacy.
Area of Science:
- Nanomedicine
- Drug Delivery Systems
- Oncology
Background:
- Efficient and site-specific delivery of cancer therapeutics remains a significant clinical challenge.
- Nanocarriers like liposomes and nanoparticles enhance drug bioavailability and pharmacokinetics, partly via the enhanced permeability and retention (EPR) effect.
- Targeting ligands conjugated to nanocarriers enable selective delivery to tumor cells or vasculature, improving therapeutic outcomes.
Purpose of the Study:
- To review recent advancements in the development of targeted nanocarriers for cancer therapy.
- To introduce novel concepts including multi-targeting and multi-functional nanoparticles.
- To highlight strategies for improving drug bioavailability and achieving site-specific delivery.
Main Methods:
- Review of literature on targeted nanocarrier development.
- Analysis of various targeting ligands (e.g., folate, antibodies, aptamers).
- Discussion of nanoparticle functionalities for imaging and triggered release.
Main Results:
- Targeted nanocarrier delivery has demonstrated improved therapeutic responses in vitro and in vivo.
- Various ligands have been successfully employed for receptor-targeted delivery.
- Nanoparticles can be engineered with multiple functionalities for enhanced therapeutic strategies.
Conclusions:
- Targeted nanocarriers represent a promising approach for improving cancer treatment efficacy.
- Multi-targeting and multi-functional nanoparticles offer novel avenues for advanced cancer therapy.
- Further development in nanocarrier design is crucial for overcoming drug delivery challenges in oncology.
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