Development and optimization of Soluplus®/Pluronic-based polymeric micelles for bicalutamide delivery:...

Area of Science:

• Nanotechnology
• Materials Science
• Pharmaceutical Sciences

Background:

• Polymeric micelles are advanced nanocarriers for enhancing drug solubility and efficacy.
• Poorly water-soluble drugs present formulation challenges in drug delivery.
• Bicalutamide (BIC) is a key drug for prostate cancer treatment with limited solubility.

Purpose of the Study:

• To develop and optimize bicalutamide-loaded polymeric micelles.
• To evaluate the physicochemical properties, stability, and in vitro performance of these nanocarriers.
• To assess the cellular uptake and cytotoxic effects of the bicalutamide-loaded micelles in prostate cancer cells.

Main Methods:

• Formulation optimization using Central Composite Design (CCD) with Soluplus® and Pluronic ratios.
• Characterization of particle size, polydispersity index (PDI), zeta potential, and morphology via TEM.
• Assessment of encapsulation efficiency, in vitro drug release, solubility enhancement, and colloidal stability.
• In vitro cellular uptake and cytotoxicity (MTT assay) studies using PC-3 prostate cancer cells.

Main Results:

• Optimized micelles showed particle size < 100 nm, low PDI (≤ 0.066), and high encapsulation efficiency (up to 90.6%).
• Formulations demonstrated sustained drug release over 72 h and significantly increased BIC solubility (161-335-fold).
• Micelles exhibited excellent colloidal and physical stability, effective cellular uptake, and enhanced cytotoxicity against PC-3 cells, with good biocompatibility of blank micelles.

Conclusions:

• Developed polymeric micelles are stable, biocompatible, and effective nanocarriers for bicalutamide.
• These systems significantly improve bicalutamide solubility and enhance its anti-cancer efficacy.
• The optimized nanocarrier system holds potential for improved prostate cancer therapy, warranting further investigation.