Preparation and Characterization of Minoxidil Loaded Nanostructured Lipid Carriers

AAPS PharmSciTech. 2017 Feb;18(2):509-516. doi: 10.1208/s12249-016-0519-x. Epub 2016 Apr 27.

Abstract

Nanostructured lipid carriers (NLCs) are interesting delivery systems for enhancing the penetration of an active substance through the skin after topical administration. The present paper described the development of a novel NLCs for minoxidil (MXD) topical delivery. Stearic acid and oleic acid that showed the highest solubility for MXD were selected as solid lipid and liquid lipid, respectively, and the NLCs were prepared by hot high pressure homogenization method. The minoxidil loaded NLCs prepared accordingly to the optimal formulation exhibited spherical shape with a mean diameter of 281.4 ± 7.4 nm, polydispersity of 0.207 ± 0.009, zeta potential of -32.90 ± 1.23 mV, drug entrapment efficiency of 92.48 ± 0.31%, and drug loading of 13.85 ± 0.47%. Storage stability studies demonstrated that the particle size and entrapment efficiency of the MXD-NLCs were not changed during 3 months both at 4°C and room temperature. Moreover, the release of MXD from the NLCs was faster than drug release from SLNs. In vitro skin permeability test demonstrated that MXD-NLCs had a more pronounced permeation and retention profile than MXD-SLNs. Furthermore, no erythema was observed after administration of MXD-NLCs. All these results indicated that the developed MXD-NLCs could be a promising and effective nanocarrier for topical delivery of MXD.

Keywords: minoxidil; nanostructured lipid carriers; skin permeation.

MeSH terms

  • Administration, Topical
  • Animals
  • Chemistry, Pharmaceutical / methods
  • Drug Carriers / chemistry*
  • Drug Delivery Systems / methods
  • Drug Liberation
  • Lipids / administration & dosage
  • Lipids / chemistry*
  • Male
  • Minoxidil / administration & dosage
  • Minoxidil / chemistry*
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry
  • Nanostructures / administration & dosage
  • Nanostructures / chemistry*
  • Particle Size
  • Permeability
  • Rats
  • Rats, Sprague-Dawley
  • Skin / metabolism

Substances

  • Drug Carriers
  • Lipids
  • Minoxidil