Leuprolide Acetate

Leuprolide acetate directly regulated extracellular matrix production in human leiomyoma cells through GnRH receptor-mediated pathways. Treatment of leiomyoma cells with leuprolide acetate for 6 hours resulted in significant increases in GnRHR1 mRNA expression, COL1A1 mRNA expression, fibronectin mRNA expression, and versican variant V0 mRNA expression. At lower concentrations, leuprolide acetate produced a dose-responsive increase in versican variant V0 expression. However, leuprolide treatment at higher concentrations did not result in increased protein production. No significant alterations in leiomyoma cell proliferation were observed following leuprolide acetate treatment. These findings demonstrated that GnRH agonists directly regulate the expression of extracellular matrix components in leiomyoma cells through GnRH receptor activation, independent of their effects on the pituitary-gonadal axis.

Fig. 1 Effects of leuprolide treatment on GnRHR1 gene expression and protein production in leiomyoma cells. (Britten J L.; et al. 2012)

An amphiphilic leuprolide acetate-oleic acid conjugate was synthesized to form self-assembled nanoparticles with uniformly spherical morphology and particle sizes ranging from 130.6 to 159.1 nm. Docetaxel-encapsulating nanoparticles were also developed for triple-synergistic drug delivery. The nanoparticles exhibited excellent membrane permeability and high lymphatic uptake potential. Leuprolide acetate and docetaxel were released in a controlled manner for 7 days. In cytotoxicity assays, the docetaxel-loaded nanoparticles exhibited significantly higher cytotoxicity against PC3 human prostate cancer cells than either drug alone, while no significant cytotoxicity was observed in normal human fibroblast cells. Confocal microscopy confirmed cellular uptake of the nanoparticles in both PC3 and macrophage cells.

Fig. 2 Preparation and characterization of leuprolide acetate-loaded self-assembled nanoparticles. (Lee J.; et al. 2025)