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PLGA-PEG Nanoparticles Loaded with Cdc42 Inhibitor for Colorectal Cancer Targeted Therapy
Sanazar Kadyr1, Altyn Zhuraliyeva2, Aislu Yermekova2
1School of Medicine, Nazarbayev University, 010000 Astana, Kazakhstan.
Abstract:
Background/Objectives: An inhibitor of small Rho GTPase Cdc42, CASIN, has been shown to reduce cancer cell proliferation, migration, and invasion, yet it has several limitations, including rapid drug elimination and low bioavailability, which prevents its systemic administration. In this study, we designed and characterized a nanoparticle-based delivery system for CASIN encapsulated within poly(lactide-co-glycolide)-block-poly(ethylene glycol)-carboxylic acid endcap nanoparticles (PLGA-PEG-COOH NPs) for targeted inhibition of Cdc42 activity in colon cancer. Methods: We applied DLS, TEM, and UV-vis spectroscopy methods to characterize the size, polydispersity index, zeta potential, encapsulation efficiency, loading capacity, and in vitro drug release of the synthesized nanoparticles. The CCK-8 cell viability test was used to study colorectal cancer cell growth in vitro. Results: We showed that CASIN-PLGA-PEG-COOH NPs were smooth, spherical, and had a particle size of 86 ± 1 nm, with an encapsulation efficiency of 66 ± 5% and a drug-loading capacity of 5 ± 1%. CASIN was gradually released from NPs, reaching its peak after 24 h, and could effectively inhibit the proliferation of HT-29 (IC50 = 19.55 µM), SW620 (IC50 = 9.33 µM), and HCT116 (IC50 = 10.45 µM) cells in concentrations ranging between 0.025-0.375 mg/mL. CASIN-PLGA-PEG-COOH NPs demonstrated low hemolytic activity with a hemolytic ratio of less than 1% for all tested concentrations. Conclusion: CASIN-PLGA-PEG-COOH NPs have high encapsulation efficiency, sustained drug release, good hemocompatibility, and antitumor activity in vitro. Our results suggest that PLGA-PEG-COOH nanoparticles loaded with CASIN show potential as a targeted treatment for colorectal cancer and could be recommended for further in vivo evaluation.
Insights
Researchers developed nanoparticle drug delivery for CASIN, an inhibitor of Cdc42, to treat colon cancer. The new system shows sustained release and effective in vitro antitumor activity, suggesting potential for targeted colorectal cancer therapy.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Cancer Research
Background:
- CASIN, a Cdc42 inhibitor, shows promise against cancer but suffers from poor bioavailability and rapid elimination.
- Current limitations of CASIN hinder its systemic administration for cancer treatment.
- Targeted delivery systems are needed to overcome CASIN's pharmacokinetic challenges.
Purpose of the Study:
- To design and characterize poly(lactide-co-glycolide)-block-poly(ethylene glycol)-carboxylic acid (PLGA-PEG-COOH) nanoparticles for CASIN delivery.
- To evaluate the in vitro antitumor efficacy and hemocompatibility of CASIN-loaded PLGA-PEG-COOH nanoparticles.
- To assess the potential of this nanoparticle system for targeted colorectal cancer therapy.
Main Methods:
- Nanoparticle characterization using Dynamic Light Scattering (DLS), Transmission Electron Microscopy (TEM), and UV-vis spectroscopy.
- Assessment of encapsulation efficiency, drug loading capacity, and in vitro drug release kinetics.
- In vitro cytotoxicity evaluation via CCK-8 assay on colorectal cancer cell lines (HT-29, SW620, HCT116) and hemolytic activity testing.
Main Results:
- CASIN-PLGA-PEG-COOH nanoparticles exhibited a spherical morphology, particle size of 86 ± 1 nm, 66 ± 5% encapsulation efficiency, and 5 ± 1% drug loading capacity.
- Sustained release of CASIN from nanoparticles was observed, peaking after 24 hours.
- Effective inhibition of colorectal cancer cell proliferation was demonstrated in vitro, with low hemolytic activity (<1%).
Conclusions:
- CASIN-PLGA-PEG-COOH nanoparticles demonstrate high encapsulation efficiency, sustained drug release, and favorable hemocompatibility.
- The developed nanoparticles show significant in vitro antitumor activity against colorectal cancer cells.
- CASIN-loaded PLGA-PEG-COOH nanoparticles represent a promising platform for targeted colorectal cancer treatment, warranting further in vivo investigation.
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