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Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?
Published on: June 13, 2014
Recent progress on charge-reversal polymeric nanocarriers for cancer treatments
Qingmei Sun1, Yunqing Zhu1,2, Jianzhong Du1,2
1Department of Polymeric Materials, School of Materials Science and Engineering, Key Laboratory of Advanced Civil Engineering Materials of Ministry of Education, Tongji University, 4800 Caoan Road, Shanghai 201804, People's Republic of China.
Abstract:
Nanocarriers (NCs) for delivery anticancer therapeutics have been under development for decades. Although great progress has been achieved, the clinic translation is still in the infancy. The key challenge lies in the biological barriers which lie between the NCs and the target spots, including blood circulation, tumor penetration, cellular uptake, endo-/lysosomal escape, intracellular therapeutics release and organelle targeting. Each barrier has its own distinctive microenvironment and requires different surface charge. To address this challenge, charge-reversal polymeric NCs have been a hot topic, which are capable of overcoming each delivery barrier, by reversing their charges in response to certain biological stimuli in the tumor microenvironment. In this review, the triggering mechanisms of charge reversal, including pH, enzyme and redox approaches are summarized. Then the corresponding design principles of charge-reversal NCs for each delivery barrier are discussed. More importantly, the limitations and future prospects of charge-reversal NCs in clinical applications are proposed.
Insights
Charge-reversal nanocarriers offer a promising strategy to overcome biological barriers in cancer therapy delivery. This review explores their design, triggering mechanisms, and clinical potential.
Area of Science:
- Biomedical Engineering
- Materials Science
- Nanotechnology
Background:
- Nanocarriers (NCs) are crucial for delivering anticancer therapeutics, but clinical translation is hindered by biological barriers.
- These barriers include navigating blood circulation, tumor penetration, cellular uptake, endosomal escape, and intracellular drug release.
Purpose of the Study:
- To review the development and application of charge-reversal polymeric nanocarriers for overcoming biological barriers in cancer therapy.
- To summarize triggering mechanisms and design principles for effective nanocarrier-based drug delivery.
Main Methods:
- This review summarizes existing literature on charge-reversal nanocarriers.
- It discusses stimuli-responsive mechanisms (pH, enzyme, redox) and their impact on nanocarrier design.
- The review analyzes how these nanocarriers address specific biological barriers.
Main Results:
- Charge-reversal nanocarriers demonstrate potential in overcoming multiple delivery barriers by adapting their surface charge.
- pH, enzyme, and redox stimuli are key triggers for charge reversal in the tumor microenvironment.
- Specific design strategies can enhance nanocarrier performance for each barrier.
Conclusions:
- Charge-reversal nanocarriers represent a significant advancement in overcoming nanocarrier delivery challenges for cancer therapeutics.
- Further research into their limitations and clinical prospects is essential for successful translation.
- Optimized design and understanding of tumor microenvironment interactions are key for future applications.

