Rutin and quercetin gastro-resistant microparticles obtained by spray-drying technique

Quercetin and rutin gastro-resistant microparticles were prepared by spray-drying using cellulose acetate trimellitate (CAT) or cellulose acetate phthalate (CAP) as coating polymers. The influence of parameters such as the initial organic or aqueous feed solutions and polymer/drug ratio on the particle yield, behaviour and morphology was investigated. By spray-drying 2% buffer aqueous feed solutions in different polymer/drug ratio (1:1, 3:1 and 5:1) microparticles loaded with rutin were obtained. The microsystems were characterized by scanning electron microscopy (SEM), fluorescence microscopy (FM), and differential scanning calorimetry (DSC). In vitro dissolution studies, carried out using a pH change method, showed a typical biphasic drug release trend due to the pH dependent solubility of the enteric polymers.

[1]  S. Wolffram,et al.  Bioavailability and metabolism of the flavonol quercetin in the pig. , 2000, Free radical biology & medicine.

[2]  K. Barrett,et al.  Effects of quercetin on epithelial chloride secretion. , 1997, Life sciences.

[3]  M. Alcaraz,et al.  Anti-inflammatory activity and inhibition of arachidonic acid metabolism by flavonoids , 1991, Agents and Actions.

[4]  P. Giunchedi,et al.  Spray-drying as a preparation method of microparticulate drug delivery systems: an overview , 1995 .

[5]  C. Rice-Evans,et al.  The small intestine can both absorb and glucuronidate luminal flavonoids , 1999, FEBS letters.

[6]  M. Amorim,et al.  Microparticles for delivering therapeutic peptides and proteins to the lumen of the small intestine. , 2001, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[7]  L. Pelzer,et al.  Anti-inflammatory properties of plant flavonoids. Effects of rutin, quercetin and hesperidin on adjuvant arthritis in rat. , 2001, Farmaco.

[8]  O. Texier,et al.  Bioavailability of rutin and quercetin in rats , 1997, FEBS letters.

[9]  R. O. Macêdo,et al.  Thermal characterization of the quercetin and rutin flavonoids , 2002 .

[10]  L. Maggi,et al.  Fast- and Slow-Release Tablets for Oral Administration of Flavonoids: Rutin and Quercetin , 2002, Drug development and industrial pharmacy.

[11]  D. Faulds,et al.  Hydroxyethylrutosides , 1992, Drugs.

[12]  J. Ferreira,et al.  Effect of drug properties on the release from CAP microspheres prepared by a solvent evaporation method. , 1999, Journal of microencapsulation.

[13]  Johanna T. Dwyer,et al.  Flavonoids: Dietary occurrence and biochemical activity , 1998 .

[14]  P. Giunchedi,et al.  Cellulose microparticles in drug delivery , 1997 .

[15]  S. Kuo.  Antiproliferative potency of structurally distinct dietary flavonoids on human colon cancer cells. , 1996, Cancer letters.

[16]  L. Maggi,et al.  Cellulose acetate trimellitate ethylcellulose blends for non-steroidal anti-inflammatory drug (NSAID) microspheres. , 1996, Journal of microencapsulation.