Development of oral site-specific pellets containing flavonoid extract with antioxidant activity

Eur J Pharm Sci. 2016 Dec 1:95:161-169. doi: 10.1016/j.ejps.2016.10.029. Epub 2016 Oct 29.

Abstract

Herbal medicines are recognized as an effective treatment of common diseases, mainly associated with oxidative stress. Therefore developing drug delivery systems of these biological active ingredients are gaining interest. Parsley (Petroselinum crispum L.) is a well-known culinary herb and its leaf contains high amount of apigenin, therefore it is suitable as a natural source of this flavonoid. Apigenin possess many health effects such as antioxidant, anti-inflammatory and anticancer activities. Unfortunately, these benefits are limited due to the low water solubility and bioavailability, it was recently classified as BCS II group compound. Therefore the aim of this study was to develop a carrier system for Petroselinum crispum extract, containing high amount of apigenin. Microcrystalline cellulose inert pellet cores were chosen and enteric coatings were applied. The produced multiparticulates had spherical shape, narrow size distribution and low moisture content. 10% (w/w) Eudragit® L 30 D-55 and 15% (w/w) Eudragit® FS 30 D coating was adequate for the modified release in vitro. The layered pellets demonstrated antioxidant activity. It was concluded that development of oral site-specific pellets containing flavonoid extract successful and the therapeutic effectiveness could be hypothesized.

Keywords: Antioxidant activity; Apigenin; Colon specific drug delivery; Eudragit®; Flavonoid; Modified release; Pellet.

MeSH terms

  • Antioxidants / chemistry*
  • Apigenin / chemistry*
  • Biological Availability
  • Cellulose / chemistry
  • Chemistry, Pharmaceutical
  • Chromatography, High Pressure Liquid
  • Drug Delivery Systems*
  • Drug Liberation
  • Petroselinum / chemistry
  • Plant Extracts / chemistry*
  • Plant Leaves / chemistry
  • Polymethacrylic Acids / chemistry
  • Solubility
  • Spectrometry, Mass, Electrospray Ionization

Substances

  • Antioxidants
  • Plant Extracts
  • Polymethacrylic Acids
  • methylmethacrylate-methacrylic acid copolymer
  • Apigenin
  • Cellulose
  • microcrystalline cellulose