PLGA microspheres containing bee venom proteins for preventive immunotherapy

Int J Pharm. 2012 Feb 14;423(1):124-33. doi: 10.1016/j.ijpharm.2011.02.027. Epub 2011 Feb 26.

Abstract

Bee venom (BV) allergy is potentially dangerous for allergic individuals because a single bee sting may induce an anaphylactic reaction, eventually leading to death. Currently, venom immunotherapy (VIT) is the only treatment with long-lasting effect for this kind of allergy and its efficiency has been recognized worldwide. This therapy consists of subcutaneous injections of gradually increasing doses of the allergen. This causes patient lack of compliance due to a long time of treatment with a total of 30-80 injections administered over years. In this article we deal with the characterization of different MS-PLGA formulations containing BV proteins for VIT. The PLGA microspheres containing BV represent a strategy to replace the multiple injections, because they can control the solute release. Physical and biochemical methods were used to analyze and characterize their preparation. Microspheres with encapsulation efficiencies of 49-75% were obtained with a BV triphasic release profile. Among them, the MS-PLGA 34kDa-COOH showed to be best for VIT because they presented a low initial burst (20%) and a slow BV release during lag phase. Furthermore, few conformational changes were observed in the released BV. Above all, the BV remained immunologically recognizable, which means that they could continuously stimulate the immune system. Those microspheres containing BV could replace sequential injections of traditional VIT with the remarkable advantage of reduced number of injections.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adsorption
  • Antibodies / immunology
  • Antigen-Antibody Reactions / immunology
  • Bee Venoms / administration & dosage*
  • Bee Venoms / chemistry
  • Bee Venoms / immunology
  • Bee Venoms / pharmacokinetics
  • Biological Availability
  • Desensitization, Immunologic / methods*
  • Drug Stability
  • Enzyme-Linked Immunosorbent Assay
  • Humans
  • Insect Proteins / administration & dosage*
  • Insect Proteins / chemistry
  • Insect Proteins / immunology
  • Insect Proteins / pharmacokinetics
  • Lactic Acid / chemistry*
  • Microscopy, Electron, Scanning
  • Microspheres*
  • Particle Size
  • Polyglycolic Acid / chemistry*
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyvinyl Alcohol / chemistry
  • Porosity
  • Protein Binding
  • Protein Conformation
  • Spectrometry, Fluorescence
  • Surface Properties

Substances

  • Antibodies
  • Bee Venoms
  • Insect Proteins
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Polyvinyl Alcohol