Carboxylated Mesoporous Carbon Nanoparticles as Bicalutamide Carriers with Improved Biopharmaceutical and Chemo-Photothermal Characteristics

  • Molecules. 2025 Jul 22;30(15):3055. doi: 10.3390/molecules30153055.
Teodora Popova  1 Borislav Tzankov  1 Marta Slavkova  1 Yordan Yordanov  2 Denitsa Stefanova  2 Virginia Tzankova  2 Diana Tzankova  3 Ivanka Spassova  4 Daniela Kovacheva  4 Christina Voycheva  1
Affiliations
  • 1. Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Medical University of Sofia, 1000 Sofia, Bulgaria.
  • 2. Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University of Sofia, 1000 Sofia, Bulgaria.
  • 3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Medical University of Sofia, 1000 Sofia, Bulgaria.
  • 4. Institute of General and Inorganic Chemistry, Bulgarian Academy of Sciences, 1000 Sofia, Bulgaria.
Abstract

Prostate Cancer is a serious, life-threatening condition among men, usually requiring long-term chemotherapy. Due to its high efficacy, bicalutamide, a non-steroidal anti-androgen, has widespread use. However, its poor water solubility, low oral bioavailability, and nonspecific systemic exposure limit its application. To overcome these obstacles, our study explored the potential of non-carboxylated and carboxylated mesoporous carbon nanoparticles (MCN) as advanced drug carriers for bicalutamide (MCN/B and MCN-COOH/B). The physicochemical properties and release behaviour were thoroughly characterized. Functionalization with carboxylic groups significantly improved wettability, dispersion stability, as well as loading efficiency due to enhanced hydrogen bonding and π-π stacking interactions. Moreover, all systems exhibited sustained and near-infrared (NIR) triggered drug release with reduced burst-effect, compared to the release of free bicalutamide. Higher particle size and stronger drug-carrier interactions determined a zero-order kinetics and notably slower release rate of MCN-COOH/B compared to non-functionalized MCN. Cytotoxicity assays on LNCaP prostate Cancer cells demonstrated that both MCN/B and MCN-COOH/B possessed comparable antiproliferative activity as free bicalutamide, where MCN-COOH/B exhibited superior efficacy, especially under NIR exposure. These findings suggest that MCN-COOH nanoparticles could be considered as a prospective platform for controlled, NIR-accelerated delivery of bicalutamide in prostate Cancer treatment.

Keywords
bicalutamide; drug delivery; encapsulation; functionalization; mesoporous carbon nanoparticles; photothermal therapy; prostate cancer.
Products