Development of Halobetasol-loaded nanostructured lipid carrier for dermal administration: Optimization, physicochemical and biopharmaceutical behavior, and therapeutic efficacy

Nanomedicine. 2019 Aug:20:102026. doi: 10.1016/j.nano.2019.102026. Epub 2019 Jun 4.

Abstract

Halobetasol propionate (HB) is considered a super potent drug in the group of topical corticosteroids. HB has anti-inflammatory activity, vasoconstriction properties, and due to its high skin penetration, it can cause systemic side effects. To improve its characteristics, enhance topical effectiveness and reduce penetration to systemic circulation, a study to optimize and characterize a HB-loaded lipid nanocarrier (HB-NLC) has been made by high-pressure homogenization method. The formulation is composed by HB, surfactant, glyceryl distearate and capric glycerides. The optimized HB-NLC containing 0.01% of HB and 3% of total lipid shows an average size below 200 nm with a polydispersity index ≪0.2 and an encapsulation efficiency ≫90%. The in vitro and in vivo tests indicate that the HB-NLC is not toxic, is well tolerated and has an anti-inflammatory effect because they decrease the production of Interleukins in keratinocytes and monocytes. HB-NLC is considered an alternative treatment for skin inflammatory disorders.

Keywords: Corticosteroids; Halobetasol; Inflammation; Lipid nanocarrier; Skin diseases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Anti-Inflammatory Agents / pharmacology
  • Cell Death / drug effects
  • Clobetasol / administration & dosage
  • Clobetasol / analogs & derivatives*
  • Clobetasol / pharmacology
  • Drug Carriers / chemistry*
  • Female
  • Humans
  • Lipids / chemistry*
  • Male
  • Nanostructures / chemistry*
  • Nanostructures / ultrastructure
  • Rabbits
  • THP-1 Cells
  • Treatment Outcome

Substances

  • Anti-Inflammatory Agents
  • Drug Carriers
  • Lipids
  • halobetasol
  • Clobetasol