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Development of ROS-responsive amino acid-based poly(ester amide) nanoparticle for anticancer drug delivery
1Biomedical Engineering Field, and Fiber Science Program, Department of Fiber Science and Apparel Design, Cornell University, Ithaca, New York, USA.
Abstract:
Reactive oxygen species (ROS) play an important role in cellular metabolism and many oxidative stress related diseases. Oxidative stress results from toxic effects of ROS and plays a critical role in the pathogenesis of a variety of diseases like cancers and many important biological processes. It is known that the unique feature of high intracellular ROS level in cancer cells can be considered as target and utilized as a useful cancer-related stimulus to mediate intracellular drug delivery. Therefore, biomaterials responsive to excess level of ROS are of great importance in biomedical applications. In this study, a novel ROS-responsive polymer based on L-methionine poly(ester amide) (Met-PEA-PEG) was designed, synthesized, characterized and self-assembled into nano-micellar-type nanoparticles (NP). The Met-PEA-PEG NP exhibited responsiveness to an oxidative environment. The size and morphology of the nanoparticle changed rapidly in the presence of H2 O2 . The Nile Red dye was loaded into the Met-PEA-PEG NP to demonstrate a H2 O2 concentration induced time-dependent release behavior. The Met-PEA-PEG NP was sensitive to high intracellular ROS level of PC3 prostate cancer cells. Furthermore, the Met-PEA-PEG NP was investigated as a carrier of a Chinese medicine-based anticancer component, gambogic acid (GA). Compared to free GA, the GA-loaded nanocomplex (GA-NP) showed enhanced cytotoxicity toward PC3 and HeLa cells. The GA-NP also induced a higher level of apoptosis and mitochondrial depolarization in PC3 cells than free GA. The Met-PEA-PEG NP improved the therapeutic effect of GA and may serve as a potential carrier for anticancer drug delivery.
Insights
Researchers developed novel nanoparticles that respond to high reactive oxygen species (ROS) levels in cancer cells. These ROS-responsive nanoparticles effectively delivered an anticancer drug, gambogic acid, enhancing its therapeutic efficacy and cancer cell toxicity.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Cancer Research
Background:
- Reactive oxygen species (ROS) are crucial in cellular processes and diseases like cancer.
- Elevated intracellular ROS in cancer cells presents a unique target for drug delivery.
- ROS-responsive biomaterials are vital for targeted biomedical applications.
Purpose of the Study:
- To design and synthesize a novel ROS-responsive polymer, Met-PEA-PEG.
- To develop Met-PEA-PEG based nanoparticles (NP) for targeted drug delivery.
- To evaluate the efficacy of these nanoparticles as a carrier for the anticancer drug gambogic acid (GA).
Main Methods:
- Synthesis and characterization of L-methionine poly(ester amide)-PEG (Met-PEA-PEG) polymer.
- Self-assembly of Met-PEA-PEG into nano-micellar-type nanoparticles (NP).
- Assessment of NP responsiveness to hydrogen peroxide (H₂O₂) and intracellular ROS levels in cancer cells (PC3).
- Loading of gambogic acid (GA) into NP and evaluation of its release kinetics and cytotoxicity against PC3 and HeLa cells.
Main Results:
- Met-PEA-PEG NP demonstrated sensitivity to oxidative environments, with size and morphology changes in H₂O₂.
- Nile Red dye release from NP was dependent on H₂O₂ concentration, indicating controlled release.
- GA-loaded NP (GA-NP) exhibited enhanced cytotoxicity against PC3 and HeLa cancer cells compared to free GA.
- GA-NP induced higher apoptosis and mitochondrial depolarization in PC3 cells than free GA.
Conclusions:
- The novel Met-PEA-PEG NP is responsive to ROS, making it suitable for targeting cancer cells.
- Met-PEA-PEG NP effectively improved the therapeutic effect of gambogic acid.
- These ROS-responsive nanoparticles show potential as a drug delivery system for anticancer therapies.
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