Impact of nanostructured lipid carriers on dapsone delivery to the skin: in vitro and in vivo studies

Int J Pharm. 2019 Dec 15:572:118781. doi: 10.1016/j.ijpharm.2019.118781. Epub 2019 Nov 9.

Abstract

The main objective of this study was to develop, characterize and evaluate the potential use of dapsone-loaded nanostructured lipid carriers (NLCs) as a topical treatment for acne. Differently charged NLC formulations were successfully prepared using an emulsification/sonication method. The particle sizes ranged from 106.2 ± 5.6 nm to 151.3 ± 7.4 nm, and the NLCs possessed the predicted surface charges, depending on the emulsifier used (Tween 80, Transcutol P, or cetyltrimethylammonium bromide). The entrapment efficiencies ranged from 76.5 ± 3.8% to 91.1 ± 3.9%. Selected formulations were assessed for possible interactions, in vitro release, ex vivo skin permeation, pharmacological efficacy and safety compared with a hydroalcoholic solution. Dapsone was embedded in the lipid matrix of NLCs and behaved as controlled release system with a good occlusive effect. Dapsone-loaded cationic NLC formulation enhanced the skin permeation of dapsone, increase the amount of dapsone retained in the skin in controlled manner, and improved the anti-rosacea activity. Based on these encouraging results, cationic NLC represents a promising carrier for the safe topical delivery of dapsone.

Keywords: Acne vulgaris; Dapsone; NLCs; Skin delivery.

MeSH terms

  • Administration, Topical
  • Animals
  • Dapsone / administration & dosage*
  • Dapsone / chemistry*
  • Drug Carriers / chemistry*
  • Drug Delivery Systems / methods
  • Drug Liberation
  • Lipids / chemistry*
  • Mice
  • Nanoparticles / chemistry
  • Nanostructures / chemistry*
  • Particle Size
  • Skin / metabolism*
  • Skin Absorption

Substances

  • Drug Carriers
  • Lipids
  • Dapsone