Lapatinib-Loaded ZIF-8 Nanoparticles: A Multifunctional Drug Delivery System with Anticancer, Antibacterial, and Antioxidant Properties
Year: 2025
Type: article
Abstract: High Resolution Image Download MS PowerPoint Slide The pitfalls of conventional chemotherapy, including poor solubility, off-target toxicity, and multidrug resistance, have driven the development of nanoparticle-based delivery systems. Here, we report the facile one-pot synthesis of lapatinib-encapsulated zeolitic imidazolate framework-8 (LAP@ZIF-8) nanoparticles. The formulation achieved an encapsulation efficiency of 72.4% and a drug loading capacity of 6.6%. Comprehensive physicochemical characterization confirmed uniform hexagonal morphology (SEM), favorable hydrodynamic size (236 ± 2 nm; DLS), positive surface charge (+29 mV; ζ-potential), high crystallinity (XRD), and excellent thermal stability (TGA). LAP release was pH-responsive, with ∼77% cumulative release at pH 5.5 (tumor-mimicking) versus 43% at pH 7.4 after 96 h. Serum–protein binding (<11%) and hemolysis (<2%) assays demonstrated good biocompatibility. In vitro, LAP@ZIF-8 exhibited potent, selective cytotoxicity toward HER2-positive SK-BR-3 breast-cancer cells (72 h IC 50 = 1.2 μg mL –1 ) while sparing HER2-negative MCF-7 cells. Importantly, both free LAP and LAP@ZIF-8 were well-tolerated by nontumorigenic MCF-10A mammary epithelial cells: viability remained ≥90% at ≤1 μg mL –1 and exceeded 50% even at 100 μg mL –1, indicating that the IC 50 was not reached and providing a preliminary safety window for healthy tissues. Beyond its anticancer effects, the nanocarrier displayed broad-spectrum antibacterial activity (minimum bactericidal concentrations: 5 mg mL –1 for Staphylococcus aureus and 10 mg mL –1 for Escherichia coli ) and moderate antioxidant capacity (DPPH IC 50 = 666 μg mL –1 ). Collectively, these results position LAP@ZIF-8 as a versatile, pH-sensitive platform that combines selective anticancer efficacy with low toxicity to healthy cells alongside ancillary antibacterial and antioxidant properties suitable for multimodal therapy.
Source: ACS Omega
Authors: Ezgi Aslan, Gülşah Şanlı-Mohamed
Institution: Izmir Institute of Technology
Language: English
Subfield: Biomaterials
Field: Materials Science
Domain: Physical Sciences
Open Access status: gold
Estimated APC paid: $1,935
OpenAlex ID: W4416780537