Development and characterization of letrozole-encapsulated polymeric beads for sustained release

Pak J Pharm Sci. 2023 Sep;36(5(Special)):1627-1635.

Abstract

The study aimed to prepare and characterize biodegradable sustained-release beads of letrozole (LTZ) for treating cancerous disease. The ionotropic gelation method was used for the preparation and calcium chloride (CaCl2) was used as a gelating agent, while chitosan (CTS) and sodium alginate (NaAlg) as biodegradable polymeric matrices in the blend hydrogel beads. The beads were characterized for their size, surface morphology, drug entrapment efficiency, drug-polymer interaction and crystallinity using different analytic techniques, including optical microscopy, Scanning Electron Microscopy (SEM), UV-spectroscopy, Fourier-transform Infrared Spectroscopy (FTIR), Thermo gravimetric Analysis (TGA), Differential Scanning Calorimetry (DSC) and X-ray Diffraction Analysis (XRD) respectively. In vitro swelling studies were also applied to observe the response of these polymeric networks against different pH (at 1.2, 6.8 and 7.4 pH). The results from TGA and DSC exhibited that the components in the formulation possess better thermal stability. The XRD of polymeric networks displays a minor crystalline and significant amorphous nature. The SEM micrographs revealed that polymeric networks have uneven surfaces and grooves. Better swelling and in vitro outcomes were achieved at a high pH (6.8,7.4), which endorsed the pH-responsive characteristics of the prepared beads. Hence, beads based on chitosan and sodium alginate were successfully synthesized and can be used for the controlled release of letrozole.

MeSH terms

  • Alginates / chemistry
  • Chitosan* / chemistry
  • Delayed-Action Preparations
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / chemistry
  • Letrozole
  • Microscopy, Electron, Scanning
  • Particle Size
  • Polymers
  • Spectroscopy, Fourier Transform Infrared

Substances

  • Delayed-Action Preparations
  • Letrozole
  • Chitosan
  • Polymers
  • Alginates
  • Hexuronic Acids
  • Glucuronic Acid