Magnetic mesoporous silica nanoparticles as a theranostic approach for breast cancer: Loading and release of the poorly soluble drug exemestane

Int J Pharm. 2022 May 10:619:121711. doi: 10.1016/j.ijpharm.2022.121711. Epub 2022 Apr 1.

Abstract

Exemestane has a limited aqueous solubility that leads to a very high variability in absorption when administrated orally. It is crucial to develop strategies to increase the solubility and bioavailability of this drug. To overcome these issues, the aim of the present work was the development of magnetic silica mesoporous nanoparticles (IOMSNs) to carry and release exemestane. Furthermore, these nanoparticles could be also used as Magnetic Resonance Imaging (MRI) contrast agents for treatment monitorization and tumor detection. MRI analysis showed that IOMSNs present a concentration dependent contrast effect, revealing their potential for MRI applications. Also, IOMSNs present a very good polydispersity (0.224) and nanometric range size (137.2 nm). It was confirmed that the nucleus is composed by magnetite and the silica coating presents tubes with MCM-41-like hexagonal structure. Both iron oxide nanoparticles and iron oxide mesoporous silica nanoparticles were not toxic in cell culture for 24 h. Exemestane was successful released for 72 h following a typical sustained release pattern, achieving a very high loading capacity (37.7%) and in vitro release of 98.8%. Taking into account the results it is possible to conclude that IOMSNs have a high potential to be used as theranostic for intravenous breast cancer treatment with exemestane.

Keywords: Breast cancer; Exemestane; Imaging; Magnetic nanoparticles; Mesoporous silica.

MeSH terms

  • Androstadienes
  • Breast Neoplasms* / diagnostic imaging
  • Breast Neoplasms* / drug therapy
  • Contrast Media / chemistry
  • Drug Carriers / chemistry
  • Drug Liberation
  • Female
  • Humans
  • Nanoparticles* / chemistry
  • Porosity
  • Precision Medicine
  • Silicon Dioxide / chemistry

Substances

  • Androstadienes
  • Contrast Media
  • Drug Carriers
  • Silicon Dioxide
  • exemestane