Development of a topical mupirocin spray for antibacterial and wound-healing applications

Drug Dev Ind Pharm. 2017 Oct;43(10):1715-1728. doi: 10.1080/03639045.2017.1339077. Epub 2017 Jun 18.

Abstract

Objective: The aim of this study was to develop mupirocin topical spray using Eudragit E100 as a film-forming agent for the treatment of bacterial skin infections as well as to promote wound healing.

Materials and methods: Twenty-seven of mupirocin formulations were formulated containing Eudragit E100 and other excipients. Mupirocin spray was prepared by aerosol crimping and filling machine using HFA-134a as a propellant. The formulations were evaluated for their stability and physicochemical properties. The factorial study was applied to evaluate the effects of glycerol and PEG400 on mupirocin-loaded Eudragit E100 films. The optimized formulation was assessed of drug release, antibacterial activities and in vitro cell line studies in comparison to the ointment formulation.

Results and discussion: Mupirocin sprays were formulated and optimized to obtain the formulation with excellent physicochemical and mechanical properties of the dressing film. The formulation had an excellent stability up to a year with more than 80% of mupirocin content. Mupirocin was released from the film up to 90% within 2 h. The formulation had a potent antibacterial effect against S. aureus and S. epidermidis. The formulation was safe to use as a topical formulation that had no toxicity to keratinocytes, fibroblasts and monocytes. The formulation also had an antiendotoxin effect without stimulating the production of NO and inflammatory cytokines (IL-1β and TNF-α).

Conclusions: Mupirocin topical spray was successful developed as a topical formulation and can be used instead of the ointment formulation. Animal experiments are warranted to further emphasize the safe use in the human skin.

Keywords: Eudragit E100; Mupirocin; anti-infectives; biomaterials; topical spray; wound healing.

MeSH terms

  • Administration, Topical
  • Animals
  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Chemistry, Pharmaceutical
  • Humans
  • Hydrocarbons, Fluorinated / chemistry*
  • Mupirocin / administration & dosage
  • Mupirocin / chemistry
  • Mupirocin / pharmacology*
  • Staphylococcus aureus / chemistry
  • Staphylococcus aureus / drug effects*
  • Staphylococcus epidermidis / chemistry
  • Staphylococcus epidermidis / drug effects*
  • Tumor Necrosis Factor-alpha / chemistry
  • Tumor Necrosis Factor-alpha / pharmacology*
  • Wound Healing / drug effects*
  • Wound Healing / physiology

Substances

  • Anti-Bacterial Agents
  • Hydrocarbons, Fluorinated
  • Tumor Necrosis Factor-alpha
  • Mupirocin
  • apaflurane