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

International Journal of Biological Macromolecules
Giulia AuriemmaRita P Aquino

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.

Citations

Jul 16, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Giulia AuriemmaRita Patrizia Aquino
Mar 8, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Paola RussoRita P Aquino
Jun 21, 2020·Fitoterapia·Oksana ZaitsevaTatyana Polezhaeva

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