Anti‐PSMA Functionalized PLGA‐PEG Nanoparticles for Active Targeting of LnCap Cells and Controlled Release of Docetaxel in Prostate Cancer

Polymeric nanoparticles have been well researched as drug delivery systems for chemotherapeutic drugs, and here, the development of an actively targeted nano‐system for the delivery of docetaxel to prostate cancer is described. The system was composed of poly (lactic‐ co ‐glycolic) acid, poly (ethylene glycol), and an antibody that effectively targets prostate‐specific membrane antigen (PSMA), a receptor highly expressed on the surface of the majority of prostate cancer cells. The ratio of polymers, amount of docetaxel, and amount of antibody were varied, while the yield of production, drug loading, and antibody conjugation efficiency were measured. The optimized system showed a yield of 63.2% ± 1.1%, a drug loading of 11.5% ± 0.66%, and antibody conjugation efficiency of 74.3% ± 4.6%. The in vitro release kinetic study showed a pH dependent 72.2% ± 5.5% maximum release of docetaxel, while the in vitro toxicity and uptake assays showed a high selectivity of the targeted system toward LnCap, a prostate cancer cell line that highly expresses PSMA. The targeted system also showed a 43% and 71% increase in toxicity compared to the non‐targeted system and free docetaxel, respectively. The optimized nano‐system's favorable pharmacological profile suggests its potential use as a chemotherapeutic agent in prostate cancer treatment.