Fabrication of Antimicrobial Peptide-Loaded PLGA/Chitosan Composite Microspheres for Long-Acting Bacterial Resistance

Molecules. 2017 Sep 29;22(10):1637. doi: 10.3390/molecules22101637.

Abstract

An antimicrobial decapeptide, KSL-W (KKVVFWVKFK-CONH₂), which could maintain stable antimicrobial activity in saliva, has therefore been widely used to inhibit biofilm formation on teeth and prevent the growth of oral microorganisms for related infectious diseases treatment. In order to control the release of KSL-W for long-term bacterial resistance, KSL-W-loaded PLGA/chitosan composite microspheres (KSL/PLGA/CS MSs) were prepared by electrospraying and combined crosslinking-emulsion methods. Different formulations of microspheres were characterized as to surface morphology, size distribution, encapsulation efficiency, in vitro drug release, and antimicrobial activity. Antibacterial experiment demonstrated the prolonged antimicrobial and inhibitory effects of KSL/PLGA/CS MSs on oral bacteria. Moreover, the cell proliferation assay proved that the released KSL-W antibacterial dosage had no cytotoxicity to the growth of osteoblast MC3T3-E1. Thus, our study suggested that the KSL-W-loaded PLGA/CS composite microspheres may have potentially therapeutic applications as an effective drug delivery system in the treatment of oral infectious diseases such as periodontitis and periodontitis, and also within bone graft substitutes for alveolar bone augmentation.

Keywords: PLGA; antimicrobial peptides; bacterial resistance; composite microspheres; electrospraying.

MeSH terms

  • Anti-Infective Agents / administration & dosage*
  • Antimicrobial Cationic Peptides / administration & dosage*
  • Bacteria / drug effects*
  • Biocompatible Materials / chemistry
  • Chitosan* / chemistry
  • Circular Dichroism
  • Drug Compounding
  • Drug Delivery Systems
  • Drug Liberation
  • Drug Resistance, Bacterial / drug effects*
  • Drug Stability
  • Lactic Acid* / chemistry
  • Microspheres*
  • Particle Size
  • Polyglycolic Acid* / chemistry
  • Polylactic Acid-Polyglycolic Acid Copolymer

Substances

  • Anti-Infective Agents
  • Antimicrobial Cationic Peptides
  • Biocompatible Materials
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Chitosan