Development and evaluation of choline tagged mesoporous silica nanoparticles for targeted delivery and imaging in prostate cancer.

This study presents MSNCHDT@DTX, mesoporous silica nanoparticles (MSN) functionalized with choline and diethylenetriaminepentaacetic acid (DTPA), designed as a theranostic agent integrating targeting, imaging, and therapy. Docetaxel (DTX) use in prostate cancer is limited by poor water solubility and systemic toxicity. Exploiting elevated choline uptake in PC-3 cells, MSN were covalently functionalized with choline and DTPA, with DTX subsequently encapsulated within the mesoporous framework. Structure elucidating techniques confirmed successful synthesis, while comprehensive physicochemical characterization validated the grafting of choline and DTPA onto the nanoparticle surface and confirmed drug encapsulation. The system demonstrated stability under physiological conditions and high selectivity for PC-3 human prostate cancer cells, achieving ∼88% increased cellular uptake. Cytotoxic activity surpassed that of both non-targeted nanoparticles and the free drug, with an IC50 of 20 μg/mL at 48 h. By selectively targeting cancerous cells while sparing healthy tissue, MSNCHDT@DTX represents a promising advancement in prostate cancer theranostics.