Viscosified Solid Lipidic Nanoparticles Based on Naringenin and Linolenic Acid for the Release of Cyclosporine A on the Skin

Molecules. 2020 Aug 2;25(15):3535. doi: 10.3390/molecules25153535.

Abstract

Psoriasis is one of the most common human skin disorders. Although its pathogenesis is complex and not completely know, the hyperactivation of the immune system seem to have a key role. In this regard, among the most effective systemic therapeutics used in psoriasis, we find cyclosporine, an immunosuppressive medication. However, one of the major problems associated with the use of cyclosporine is the occurrence of systemic side effects such as nephrotoxicity, hypertension, etc. The present work fits in this context and its aim is the design of suitable platforms for cyclosporine topical release in psoriasis treatment. The main objective is to achieve local administration of cyclosporine in order to reduce its systemic absorption and, consequently, its side effects. In order to improve dermal penetration, solid lipid nanoparticles (SLNs) are used as carriers, due to their lipophilicity and occlusive properties, and naringenin and linolenic acid are chosen, due to their properties, as starting materials for SLNs design. In order to have dermatological formulations and further modulate drug release, SLNs are incorporated in several topical vehicles obtaining gels with different degree of lipophilicity. Potential applications for psoriasis treatment were evaluated by considering the encapsulation efficiency, release profiles, in vitro skin permeation, and anti-inflammatory effects.

Keywords: anti-inflammatory; antioxidant; cyclosporine A; linolenic acid; naringenin; release; skin; solid lipid nanoparticles.

MeSH terms

  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology
  • Antioxidants / chemistry
  • Antioxidants / pharmacology
  • Cyclosporine / administration & dosage*
  • Cyclosporine / chemistry
  • Cyclosporine / pharmacokinetics*
  • Drug Carriers
  • Drug Compounding
  • Drug Liberation
  • Flavanones / chemistry*
  • Humans
  • Lipids / administration & dosage
  • Lipids / chemistry*
  • Lipids / pharmacology*
  • Molecular Structure
  • Particle Size
  • Skin / drug effects*
  • Skin Absorption
  • Spectroscopy, Fourier Transform Infrared
  • alpha-Linolenic Acid / chemistry*

Substances

  • Anti-Inflammatory Agents
  • Antioxidants
  • Drug Carriers
  • Flavanones
  • Lipids
  • alpha-Linolenic Acid
  • Cyclosporine
  • naringenin