Dual-Layered, pH-Responsive PLGA-Based Nanocarriers for Enhanced Niclosamide Delivery and Anticancer Activity

Area of Science:

• Biomaterials Science
• Nanotechnology
• Cancer Therapeutics

Background:

• Niclosamide is a promising anticancer agent, but its clinical use is limited by poor aqueous solubility.
• Developing effective drug delivery systems is crucial for overcoming niclosamide's bioavailability challenges.

Purpose of the Study:

• To develop and characterize a novel dual-layered nanocarrier system, PLGA@Na-CMC-CaCO3, for improved niclosamide delivery.
• To evaluate the encapsulation efficiency, pH-responsive drug release, and in vitro anticancer activity of the developed nanocarrier.

Main Methods:

• Fabrication of PLGA@Na-CMC-CaCO3 nanocarriers encapsulating niclosamide.
• Characterization using Dynamic Light Scattering (DLS), Fourier-Transform Infrared Spectroscopy (FTIR), X-ray Diffraction (XRD), and Thermogravimetric Analysis (TGA).
• In vitro drug release studies at different pH values and cytotoxicity assays on MDA-MB-231 cells.

Main Results:

• The nanocarrier system exhibited uniform size and high encapsulation efficiency (∼95.67%).
• Demonstrated pH-responsive niclosamide release, with higher release rates at acidic pH simulating tumor microenvironments.
• Niclosamide-loaded nanocarriers showed enhanced dose-dependent cytotoxicity and induced apoptosis in cancer cells, with negligible toxicity from the nanocarrier alone.

Conclusions:

• The PLGA@Na-CMC-CaCO3 nanocarrier system effectively addresses niclosamide's solubility and delivery issues.
• This system holds significant potential for enhancing niclosamide's efficacy in cancer therapy.
• The biocompatibility and targeted release profile suggest a promising platform for future cancer treatment strategies.