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"Development, optimization, and characterization of Eudragit-based nanoparticles for Dasatinib delivery"
Hemanth G1, Anasuya Patil1, Hariprasad Mg2
1Department of Pharmaceutics, KLE College of Pharmacy, Bengaluru, India.
Journal of Biomaterials Science. Polymer Edition
|November 19, 2024
Summary
Dasatinib-loaded nanoparticles (DST-NPs) show promise for breast cancer treatment. These nanoparticles improved drug bioavailability, targeted tumors effectively, and demonstrated significant anti-cancer efficacy in preclinical models.
Area of Science:
- Nanotechnology
- Materials Science
- Oncology
Background:
- Breast cancer remains a leading cause of mortality worldwide, necessitating novel therapeutic strategies.
- Conventional chemotherapy faces challenges including poor bioavailability and off-target toxicity.
- Nanoparticle-based drug delivery systems offer potential solutions for enhancing cancer treatment efficacy.
Purpose of the Study:
- To develop and characterize dasatinib-loaded nanoparticles (DST-NPs) using Eudragit L100 for improved breast cancer therapy.
- To evaluate the in vitro and in vivo performance of DST-NPs.
- To assess the pharmacokinetic, biodistribution, efficacy, and safety profiles of DST-NPs.
Main Methods:
- Formulation of dasatinib-loaded nanoparticles (DST-NPs) using Eudragit L100.
- Characterization of DST-NPs for particle size, zeta potential, and entrapment efficiency.
- In vitro drug release, cytotoxicity assays (MTT), and stability studies.
- In vivo pharmacokinetic, tissue distribution, efficacy (DMBA-induced mammary carcinoma model), hematologic, and histopathological analyses in rats.
Main Results:
- Optimized DST-NPs showed favorable physicochemical properties (202.1 nm size, -18 mV zeta potential, 93.11% entrapment efficiency).
- Sustained in vitro drug release, enhanced in vivo bioavailability (higher Cmax and AUC0-t), and improved tumor targeting were observed.
- DST-NPs significantly reduced tumor volume, improved survival rates, exhibited favorable hematologic profiles, and restored normal tissue architecture.
- Higher cytotoxicity against breast cancer cell lines (MCF-7, MDA-MB231, 4T1) with lower IC50 values compared to pure dasatinib.
Conclusions:
- DST-NPs formulated with Eudragit L100 represent a promising nanocarrier for enhanced breast cancer treatment.
- The developed nanoparticles offer improved drug delivery, efficacy, and safety profile compared to free dasatinib.
- Further investigation into DST-NPs could lead to advanced therapeutic options for breast cancer patients.
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