Planta Med 2009; 75 - SL18
DOI: 10.1055/s-0029-1234273

Nasal formulations of a polyphenols-enriched extract of Herba Cisti

M Heinrich 1, S Rosen 1, H Gill 2, B Feistel 3, KMG Taylor 2
  • 1Centre for Pharmacognosy and Phytotherapy, School of Pharmacy, University of London, 29–39 Brunswick Square, London WC1N 1AX, UK
  • 2Department of Pharmaceutics, School of Pharmacy, University of London, 29–39 Brunswick Square, London WC1N 1AX, UK
  • 3Finzelberg GmbH & Co. KG, Koblenzer Str. 48–56, 56626 Andernach, Germany

The aqueous extract ECce20 of Cistus creticus ssp. eriocephalus, herba (CCE, previously studied as Cistus incanus) is rich in polyphenols, including flaven-3-ols and proanthocyanidins [1]. The reported antiviral and anti-inflammatory activity of some extracts [2,3] has led us to formulate and characterise a nasal formulation for local delivery using a CCE hot water extract [4], supplied by the extract company Finzelberg.

Following determination of the extract's solubility in ethanol/water solvent mixes, optimised formulations containing 1, 10, 50 and 100mg/ml powdered extract and benzalkonium chloride (0.01% w/v as preservative) in ethanol/water (5:95) were developed. Solutions were delivered as an aerosol from metered dose nasal sprays (Valois VP3). Aerosols were sized by laser diffraction; the weight of each actuation was determined by difference. Solubility and delivery of Cistus extract was determined by absorbance at 368nm using UV Spectrophotometer.

The mean size of all aerosols was in the range 40–41µm, with a weight, per actuation, of 101.5mg. These are functions of the 100µl metered dose volume. The mean delivered dose per actuation of CCE-extract over the first 55 actuations of the product was 0.088±0.062mg (1mg/ml), 1.086±0.011mg (10mg/ml), 5.494±0.175mg (50mg/ml) and 11.296±0.090mg (100mg/ml).

The developed, preserved formulation has an aerosol droplet size appropriate for nasal delivery, delivers a consistent uniformity of dose (by weight) and delivers between 88 and 113% of the nominal dose of CCE-extract per actuation for the four concentrations of extract examined.

References: [1] Danne, A. et al. (1993) Phytochemistry 34:1129–1133.

[2] Droebner, K. et al. (2007) Antivir. Res. 76:38–47.

[3] Taila, S. et al. (2008)J. Pharm. Pharmacol. 60: 62–63.

[4] Obolsky, D. (2008) Phytochemical and in vitro NF-kappa B inhibitory/Antioxidant Profiling of Cistus creticus L. subsp. eriocephalus (Viv.) Greuter & Burdet; MSc dissertation, The School of Pharmacy, University of London.