Hybrid chitosan-lipid nanoparticles of green tea extract as natural anti-cellulite agent with superior in vivo potency: full synthesis and analysis

Drug Deliv. 2021 Dec;28(1):2160-2176. doi: 10.1080/10717544.2021.1989088.

Abstract

The aim of this work is to exploit the advantages of chitosan (CS) as a nanocarrier for delivery of anti-cellulite drug, green tea extract (GTE), into subcutaneous adipose tissue. Primarily, analysis of herbal extract was conducted via newly developed and validated UPLC method. Ionic gelation method was adopted in the preparation of nanoparticles where the effect lecithin was investigated resulting in the formation of hybrid lipid-chitosan nanoparticles. Optimal formula showed a particle size of 292.6 ± 8.98 nm, polydispersity index of 0.253 ± 0.02, zeta potential of 41.03 ± 0.503 mV and an entrapment efficiency percent of 68.4 ± 1.88%. Successful interaction between CS, sodium tripolyphosphate (TPP) and lecithin was confirmed by Fourier-transform infrared spectroscopy, differential scanning calorimetry and X-ray diffraction. Morphological examination was done using transmission electron microscope and scanning electron microscope confirmed spherical uniform nature of GTE load CS-TPP nanoparticles. Ex vivo permeation study revealed permeability enhancing activity of the selected optimal formula due to higher GTE deposition in skin in comparison to GTE solution. Moreover in vivo study done on female albino Wistar rats carried out for 21 days proved successful potential anti-cellulite activity upon its application on rats' skin. Histological examination showed significant reduction of adipocyte perimeter and area and fat layer thickness. Results of the current study demonstrated that the developed GTE-loaded CS-TPP nanoparticle comprised of chitosan and lecithin showed permeability enhancing activity along with the proven lipolytic effect of green tea represent a promising delivery system for anti-cellulite activity.

Keywords: Chitosan; cellulite; green tea extract; ionic gelation; lecithin; nanocarrier.

MeSH terms

  • Adipose Tissue / drug effects*
  • Animals
  • Calorimetry, Differential Scanning
  • Chemistry, Pharmaceutical / methods
  • Chitosan / chemistry*
  • Drug Carriers / chemistry
  • Female
  • Lecithins / chemistry
  • Liposomes / chemistry*
  • Nanoparticles / chemistry*
  • Particle Size
  • Plant Extracts / administration & dosage*
  • Plant Extracts / pharmacokinetics
  • Plant Extracts / pharmacology*
  • Polyphosphates / chemistry
  • Rats
  • Rats, Wistar
  • Skin Absorption / drug effects
  • Spectroscopy, Fourier Transform Infrared
  • Surface Properties
  • Tea*
  • X-Ray Diffraction

Substances

  • Drug Carriers
  • Lecithins
  • Lipid Nanoparticles
  • Liposomes
  • Plant Extracts
  • Polyphosphates
  • Tea
  • Chitosan
  • triphosphoric acid