Development of folic acid-loaded nanostructured lipid carriers for topical delivery: preparation, characterisation and ex vivo investigation

J Microencapsul. 2020 Aug;37(5):366-383. doi: 10.1080/02652048.2020.1761904. Epub 2020 May 7.

Abstract

The present work is designed to achieve efficient localised skin delivery of folic acid (FA)-loaded nanostructured lipid carriers (NLCs) to infer efficient treatment of skin photoageing conditions induced via excessive exposure to ultraviolet (UV) radiation. FA NLCs were prepared by high-speed homogenisation followed by ultrasonication. The obtained NLCs revealed high encapsulation efficiencies (89.42-99.26%) with nanometric particle sizes (27.06-85.36 nm) of monodisperse distribution (PDI = 0.137-0.442), zeta potential values >|27| mV, pseudoplastic rheological behaviour, good spreadability (2.25-3.30 cm) and promoted occlusive properties throughout 48 h. Optimised NLC formulations appeared as sphere-shaped particles using transmission electron microscopy, showed improved photostability of FA and prolonged in vitro release profile best fitted to Higuchi diffusion model. Ex vivo permeation and deposition of FA, employing Wistar rat skins, depicted enhanced permeability and existence of FA in skin layers after 6 h. Based on the obtained results, FA-loaded NLC formulations demonstrate a promising modality for anti-photoageing therapy.

Keywords: Folic acid; nanostructured lipid carrier; occlusion; skin deposition; skin permeation; spreadability; topical delivery.

MeSH terms

  • Animals
  • Antioxidants
  • Calorimetry, Differential Scanning
  • Drug Carriers*
  • Drug Liberation
  • Folic Acid / administration & dosage*
  • Kinetics
  • Lipids / chemistry*
  • Male
  • Microscopy, Electron, Transmission
  • Nanomedicine / methods*
  • Nanostructures
  • Particle Size
  • Permeability
  • Rats
  • Rats, Wistar
  • Rheology
  • Skin Absorption
  • Ultraviolet Rays
  • Viscosity

Substances

  • Antioxidants
  • Drug Carriers
  • Lipids
  • Folic Acid