Skin-controlled release lipid nanosystems of pranoprofen for the treatment of local inflammation and pain

Nanomedicine (Lond). 2018 Oct;13(19):2397-2413. doi: 10.2217/nnm-2018-0195. Epub 2018 Oct 12.

Abstract

Aim: The design and development of pranoprofen (PF) nanostructured lipid carriers (NLCs) for topical treatment of local inflammation and pain.

Materials & methods: PF-NLCs were designed and optimized by central rotatable composite design. A physicochemical characterization was addressed. Release and skin permeation were performed in Franz diffusion cells. In vivo anti-inflammatory efficacy was assayed in mice and tolerance study in humans.

Results: PF-NLCs F7 and F10 provided sustained release, good stability and optimal skin retention avoiding systemic undesired side effects. Anti-inflammatory activity was enhanced, suggesting an improved efficacy as compared with standard formulation. No skin irritancy was detected.

Conclusion: Topical PF-NLCs F7 and F10 could be effective and safe new therapeutic tools for the treatment of local inflammation and pain. [Formula: see text].

Keywords: anti-inflammatory efficacy; dermal delivery; experimental design; inflammation; local action; nanostructured lipid carriers; osteoarthritis; pranoprofen; skin irritation; skin permeation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Topical
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage*
  • Benzopyrans / administration & dosage*
  • Benzopyrans / chemistry
  • Delayed-Action Preparations
  • Drug Carriers / chemistry
  • Humans
  • Inflammation / drug therapy*
  • Inflammation / pathology
  • Lipids / administration & dosage
  • Lipids / chemistry
  • Mice
  • Nanoparticles / administration & dosage*
  • Nanoparticles / chemistry
  • Nanostructures / chemistry
  • Propionates / administration & dosage*
  • Propionates / chemistry
  • Skin / drug effects
  • Skin Absorption / drug effects

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Benzopyrans
  • Delayed-Action Preparations
  • Drug Carriers
  • Lipids
  • Propionates
  • pyranoprofen