Preparation and characterization of lipid based nanosystems for topical delivery of quercetin

Eur J Pharm Sci. 2013 Feb 14;48(3):442-52. doi: 10.1016/j.ejps.2012.12.005. Epub 2012 Dec 13.

Abstract

The main objective of this study was to evaluate the potential of lipid nanosystems for topical delivery of the naturally occurring flavonoid quercetin. These lipid based nanosystems were manufactured using a solvent free probe ultrasonication process. Formulation factors such as the nature of the lipid (solid/combination of solid and liquid) in solid lipid nanoparticle (SLN) and nanostructured lipid carrier (NLC) systems and drug loading were evaluated to produce an optimum formulation with adequate physical stability for up to 14 weeks at 2-8°C. The mean particle size of the optimized formulation was around 282 nm, with a zeta potential value of -36.57 ± 2.67 mV, indicating the formation of a stable system. Release studies showed a biphasic release profile, characterized by an initial burst release followed by a more controlled release pattern from both SLN and NLC systems. The NLC system showed the highest improvement in topical delivery of quercetin manifested by the amount of quercetin retained in full thickness human skin, compared to a control formulation with similar composition and particle size in the micrometer range. This study demonstrated the feasibility of nanostructured lipid carrier systems for improved topical delivery of quercetin.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Cutaneous
  • Administration, Topical
  • Antioxidants / administration & dosage
  • Antioxidants / chemistry*
  • Antioxidants / metabolism
  • Dermatologic Agents / administration & dosage
  • Dermatologic Agents / chemistry*
  • Dermatologic Agents / metabolism
  • Dioctyl Sulfosuccinic Acid / chemistry
  • Drug Compounding
  • Drug Delivery Systems*
  • Drug Stability
  • Excipients / chemistry*
  • Fatty Acids / chemistry
  • Feasibility Studies
  • Humans
  • In Vitro Techniques
  • Nanostructures / chemistry*
  • Nanotechnology
  • Oleic Acid / chemistry
  • Permeability
  • Polysorbates / chemistry
  • Quercetin / administration & dosage
  • Quercetin / chemistry*
  • Quercetin / metabolism
  • Skin / chemistry
  • Skin / metabolism
  • Skin Absorption
  • Surface-Active Agents / chemistry*
  • Ultrasonics / methods

Substances

  • Antioxidants
  • Dermatologic Agents
  • Excipients
  • Fatty Acids
  • Polysorbates
  • Surface-Active Agents
  • Dioctyl Sulfosuccinic Acid
  • glyceryl behenate
  • Oleic Acid
  • Quercetin