Mesoporous silica pellets as bifunctional bone drug delivery system for cefazolin

Int J Pharm. 2020 Oct 15:588:119718. doi: 10.1016/j.ijpharm.2020.119718. Epub 2020 Aug 1.

Abstract

For decades, bone drug delivery systems dedicated for osteomyelitis treatment have been investigated as bifunctional materials that exhibit prolonged drug release and mineralization potential. Herein, composite-type pellets based on cefazolin-loaded amino-modified mesoporous silica SBA-15 and microwave-assisted hydroxyapatite were investigated as potential bone drug delivery system in vitro. Pellets were obtained by granulation, extrusion and spheronization methods in laboratory scale and studied in terms of physical properties, drug release, mineralization potential, antimicrobial activity and cytotoxicity towards human osteoblasts. The obtained pellets were characterized for hardness and friability which indicated the pellets durability during further investigations. Prolonged (5-day) release of cefazolin from pellets was observed. The pellets exhibited mineralization potential in simulated body fluid, i.e., a continuous layer of bone-like apatite was formed on the surface of pellets after 28 days of incubation. An antimicrobial assay of pellets revealed an antibacterial effect against Staphylococcus aureus strain during 6 days. No cytotoxic effects of pellets towards human osteoblasts were observed. The obtained results proved that proposed pellets appear to have potential applications as bone drug delivery systems.

Keywords: Cefazolin; Hydroxyapatite; Mesoporous silica; Osteomyelitis; Pellets.

MeSH terms

  • Anti-Bacterial Agents / administration & dosage
  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / toxicity
  • Cefazolin / administration & dosage
  • Cefazolin / chemistry*
  • Cefazolin / toxicity
  • Cell Line
  • Delayed-Action Preparations
  • Drug Carriers*
  • Drug Compounding
  • Drug Implants
  • Drug Liberation
  • Durapatite / chemistry
  • Hardness
  • Humans
  • Kinetics
  • Osteoblasts / drug effects
  • Osteomyelitis / drug therapy
  • Osteomyelitis / microbiology
  • Porosity
  • Silicon Dioxide / chemistry*
  • Silicon Dioxide / toxicity
  • Staphylococcus aureus / drug effects
  • Staphylococcus aureus / growth & development
  • Surface Properties

Substances

  • Anti-Bacterial Agents
  • Delayed-Action Preparations
  • Drug Carriers
  • Drug Implants
  • SBA-15
  • Silicon Dioxide
  • Durapatite
  • Cefazolin