Development of a skin-friendly microemulsion for dermal allergen-specific immunotherapy

Int J Pharm. 2018 Oct 25;550(1-2):463-469. doi: 10.1016/j.ijpharm.2018.09.002. Epub 2018 Sep 5.

Abstract

Due to their role in immune responses, the skin dendritic cells (i.e. epidermal Langerhans cells and dermal dendritic cells) have become of great interest to researchers in the past decades. A dermal administration of allergens could target these professional antigen-presenting cells directly and build up immunotolerance. Additionally, many of the adverse side effects, which are seen in the current state of the art specific immunotherapy routes, could be avoided. Therefore, in this study a penetration enhancing microemulsion was developed and its physicochemical properties were determined under several storage conditions. The influence of different preservatives on the microemulsion stability was observed. We examined epidermal penetration of Alexa Fluor-647 labelled bee-venom phospholipase A2 (Api m 1) using the Franz diffusion cell set up and confocal laser-scanning microscopy. First results of an in-vivo Api m 1-allergic mouse model indicated the protective efficacy of dermal AIT with our newly developed microemulsion. Summarily, the developed microemulsion is a suitable, stable drug delivery system for the topical administration of proteogenic allergens into the epidermis and is able to reach dendritic cells in the skin.

Keywords: Allergen-specific immunotherapy; Api m 1; Bee-venom phospholipase A2; Microemulsion; Skin penetration; Transdermal immunotherapy.

MeSH terms

  • Administration, Cutaneous
  • Allergens / administration & dosage*
  • Animals
  • Carbocyanines / administration & dosage
  • Desensitization, Immunologic*
  • Emulsions
  • Fluorescent Dyes / administration & dosage
  • Hypersensitivity / therapy
  • Mice
  • Preservatives, Pharmaceutical / administration & dosage
  • Skin / metabolism*
  • Skin Absorption
  • Swine

Substances

  • Alexa Fluor 647
  • Allergens
  • Carbocyanines
  • Emulsions
  • Fluorescent Dyes
  • Preservatives, Pharmaceutical