Preparation, characterization, in vitro release and degradation of cathelicidin-BF-30-PLGA microspheres

PLoS One. 2014 Jun 25;9(6):e100809. doi: 10.1371/journal.pone.0100809. eCollection 2014.

Abstract

Cathelicidin-BF-30 (BF-30), a water-soluble peptide isolated from the snake venom of Bungarus fasciatus containing 30 amino acid residues, was incorporated in poly(D,L-lactide-co-glycolide) (PLGA) 75∶25 microspheres (MS) prepared by a water in oil in water W/O/W emulsification solvent extraction method. The aim of this work was to investigate the stability of BF-30 after encapsulation. D-trehalose was used as an excipient to stabilize the peptide. The MS obtained were mostly under 2 µm in size and the encapsulation efficiency was 88.50±1.29%. The secondary structure of the peptide released in vitro was determined to be nearly the same as the native peptide using Circular Dichroism (CD). The ability of BF-30 to inhibit the growth of Escherichia coli was also maintained. The cellular relative growth and hemolysis rates were 92.16±3.55% and 3.52±0.45% respectively.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimicrobial Cationic Peptides / administration & dosage*
  • Antimicrobial Cationic Peptides / pharmacology*
  • Apoptosis / drug effects
  • Cathelicidins
  • Cell Proliferation / drug effects
  • Cells, Cultured
  • Chromatography, High Pressure Liquid
  • Circular Dichroism
  • Drug Delivery Systems*
  • Drug Stability
  • Emulsions
  • Endothelium, Vascular / cytology
  • Endothelium, Vascular / drug effects
  • Excipients
  • Hemolysis / drug effects
  • Humans
  • In Vitro Techniques
  • Lactic Acid / chemistry*
  • Microspheres*
  • Peptide Fragments / administration & dosage*
  • Peptide Fragments / pharmacology
  • Polyglycolic Acid / chemistry*
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polymers
  • Solvents / chemistry

Substances

  • Antimicrobial Cationic Peptides
  • Emulsions
  • Excipients
  • Peptide Fragments
  • Polymers
  • Solvents
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Cathelicidins

Grants and funding

This work was supported by the National Natural Science Foundation of China (31160198, 31360417), the Applied Basic Research Key Project of Yunnan (2013FA039), the Applied Basic Research Project of Yunnan (2011FB084), the High-End Technology Professionals Introduction Plan in Yunnan province (2010CI119). The funders had role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.