Design and Optimization of a Stable Lipid-Based Nanoparticulate Delivery System for Aromatase Inhibitors in Breast Cancer Therapy

Abstract

Aromatase inhibitors (AIs) represent a cornerstone in hormone receptor-positive breast cancer therapy, yet their clinical efficacy is often limited by poor aqueous solubility, low bioavailability, and systemic toxicity. Lipid-based nanoparticulate systems, including solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), and liposomes, offer promising solutions to overcome these pharmacokinetic challenges. This paper presents a comprehensive investigation into the design, formulation, characterization, and optimization of lipid nanocarriers specifically tailored for aromatase inhibitor delivery. Through systematic evaluation of formulation parameters including lipid composition, surfactant selection, preparation methods, and stabilization strategies, we demonstrate enhanced drug loading efficiency, sustained release profiles, and improved cellular uptake. The developed nanoparticulate systems exhibited particle sizes ranging from 80 to 200 nm with polydispersity indices below 0.3, encapsulation efficiencies exceeding 85%, and remarkable storage stability over six months. In vitro studies confirmed enhanced cytotoxicity against MCF-7 breast cancer cells compared to free drug formulations. This research provides a robust framework for translating lipid-based AI nanoformulations toward clinical applications, potentially improving therapeutic outcomes while minimizing adverse effects in breast cancer patients.