Polysaccharides based gastroretentive system to sustain piroxicam release: Development and in vivo prolonged anti-inflammatory effect

Abstract

A gastro-retentive delivery system loaded with piroxicam with a bimodal release profile in gastrointestinal-tract was developed.Piroxicam is characterized by high oral absorption, long half-life, but its elimination is impaired in elderly patients. To overcome fluctuations in plasma levels, floating gastro-retentive gel-beads with sustained release properties were manufactured using prilling. Beads matrix was designed as a hollow/multipolymeric system based on alginate, ALM-pectin and hydroxypropilmethylcellulose.This research studied variables able to affect particles micromeritics, hollow inner structure, floating properties and drug-release profiles in gastro-intestinal tract. The gastro-retentive formulation (F4) acted as a floating-system able to provide the desired bimodal drug-release pattern controlling and delaying in vitro piroxicam release. The in vivo anti-inflammatory activity of the floating beads resulted prolonged up to 48 h, compared to standard piroxicam.This formulation may be proposed to treat chronic inflammatory-diseases in elderly patients, needing a rapid onset of drug action followed by a maintenance dose.