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Published on: September 18, 2018
Chitosan-Coated-PLGA Nanoparticles Enhance the Antitumor and Antimigration Activity of Stattic - A STAT3 Dimerization
Stephanie Sally Fong1, Yiing Yee Foo1, Wen Shang Saw2
1Department of Pharmacology, Faculty of Medicine, University of Malaya, Kuala Lumpur, 50603, Malaysia.
Purpose:
The use of nanocarriers to improve the delivery and efficacy of antimetastatic agents is less explored when compared to cytotoxic agents. This study reports the entrapment of an antimetastatic Signal Transducer and Activator of Transcription 3 (STAT3) dimerization blocker, Stattic (S) into a chitosan-coated-poly(lactic-co-glycolic acid) (C-PLGA) nanocarrier and the improvement on the drug's physicochemical, in vitro and in vivo antimetastatic properties post entrapment.
Methods:
In vitro, physicochemical properties of the Stattic-entrapped C-PLGA nanoparticles (S@C-PLGA) and Stattic-entrapped PLGA nanoparticles (S@PLGA, control) in terms of size, zeta potential, polydispersity index, drug loading, entrapment efficiency, Stattic release in different medium and cytotoxicity were firstly evaluated. The in vitro antimigration properties of the nanoparticles on breast cancer cell lines were then studied by Scratch assay and Transwell assay. Study on the in vivo antitumor efficacy and antimetastatic properties of S@C-PLGA compared to Stattic were then performed on 4T1 tumor bearing mice.
Results:
The S@C-PLGA nanoparticles (141.8 ± 2.3 nm) was hemocompatible and exhibited low Stattic release (12%) in plasma. S@C-PLGA also exhibited enhanced in vitro anti-cell migration potency (by >10-fold in MDA-MB-231 and 5-fold in 4T1 cells) and in vivo tumor growth suppression (by 33.6%) in 4T1 murine metastatic mammary tumor bearing mice when compared to that of the Stattic-treated group. Interestingly, the number of lung and liver metastatic foci was found to reduce by 50% and 56.6%, respectively, and the average size of the lung metastatic foci was reduced by 75.4% in 4T1 tumor-bearing mice treated with S@C-PLGA compared to Stattic-treated group (p < 0.001).
Conclusion:
These findings suggest the usage of C-PLGA nanocarrier to improve the delivery and efficacy of antimetastatic agents, such as Stattic, in cancer therapy.
Insights
Chitosan-coated PLGA nanoparticles effectively delivered the antimetastatic agent Stattic, significantly reducing tumor growth and metastasis in mice. This nanocarrier system enhances drug efficacy for improved cancer therapy.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Cancer Research
Background:
- Nanocarriers are increasingly explored for drug delivery, yet their application for antimetastatic agents remains less investigated compared to cytotoxic drugs.
- Signal Transducer and Activator of Transcription 3 (STAT3) dimerization is a key pathway in cancer metastasis.
Purpose of the Study:
- To encapsulate the antimetastatic agent Stattic into chitosan-coated poly(lactic-co-glycolic acid) (C-PLGA) nanocarriers.
- To evaluate the impact of this nanocarrier system on the physicochemical, in vitro, and in vivo antimetastatic properties of Stattic.
Main Methods:
- Physicochemical characterization of Stattic-loaded C-PLGA nanoparticles (S@C-PLGA), including size, zeta potential, drug loading, and release kinetics.
- In vitro assessment of antimigratory effects on breast cancer cell lines using Scratch and Transwell assays.
- In vivo evaluation of antitumor efficacy and antimetastatic activity in 4T1 tumor-bearing mice.
Main Results:
- S@C-PLGA nanoparticles demonstrated hemocompatibility and controlled Stattic release.
- Enhanced in vitro anti-cell migration potency (>10-fold in MDA-MB-231, 5-fold in 4T1 cells) was observed.
- Significant in vivo tumor growth suppression (33.6%) and a marked reduction in lung (50%) and liver (56.6%) metastases were achieved with S@C-PLGA.
Conclusions:
- Chitosan-coated PLGA nanocarriers represent a promising platform for improving the delivery and efficacy of antimetastatic agents like Stattic.
- This nanocarrier system holds potential for enhancing cancer therapy by targeting metastasis.
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