Purpose: a) to improve dissolution rate, bioavailability and shelf-life, of Citrus Aurantium extracts from peel, pulp and seeds rich in fiber and other substances with remarkable biological compounds such as flavonoids; and b) to investigate their pharmacological properties. Methods: Gastroresistant (G-R) microsystems were obtained by spraying CAP, Sodium alginate or Eudragit feed solutions in presence of enhancers of dissolution rate. The chemical-physical properties of the raw extract and G-R formulations were evaluated by solubility studies (USP 33), UV, HPLC, DSC, FTIR, X-ray, SEM and FM analyses. The stability test was performed according ICH guidelines. Evaluation of body weight, blood glucose and cholesterol levels were performed on male CD1 mice. Effects on hepatic steatosis and changes in the expression of fats transporter CD36 in the gut were also evaluated in mice fed with a fat diet. Results: The presence of the enhancers produced well-formed microparticles containing drug well coated by the polymers. All the enhancers were able to increase the dissolution rate of extract in the simulated intestinal medium without altering protective polymers ability in the acidic fluid. The spray-drying technique and process conditions selected were effective in microencapsulating and stabilizing the flavonoids content giving satisfactory encapsulation efficiency, product yield, morphology and enteric release.. Conclusion: This approach might be suitable for delivering natural bioactive extract such as Citrus Aurantium, avoiding gastric degradation of the molecule and improving its bioavailability from solid oral dosage forms.

Gastro-resistant spray-dryed Citrus aurantium extract microsystems: improvement of dissolution rate and pharmacological activity.

LAURO, Maria Rosaria;SANSONE, FRANCESCA;PICERNO, PATRIZIA;AQUINO, Rita Patrizia;
2013

Abstract

Purpose: a) to improve dissolution rate, bioavailability and shelf-life, of Citrus Aurantium extracts from peel, pulp and seeds rich in fiber and other substances with remarkable biological compounds such as flavonoids; and b) to investigate their pharmacological properties. Methods: Gastroresistant (G-R) microsystems were obtained by spraying CAP, Sodium alginate or Eudragit feed solutions in presence of enhancers of dissolution rate. The chemical-physical properties of the raw extract and G-R formulations were evaluated by solubility studies (USP 33), UV, HPLC, DSC, FTIR, X-ray, SEM and FM analyses. The stability test was performed according ICH guidelines. Evaluation of body weight, blood glucose and cholesterol levels were performed on male CD1 mice. Effects on hepatic steatosis and changes in the expression of fats transporter CD36 in the gut were also evaluated in mice fed with a fat diet. Results: The presence of the enhancers produced well-formed microparticles containing drug well coated by the polymers. All the enhancers were able to increase the dissolution rate of extract in the simulated intestinal medium without altering protective polymers ability in the acidic fluid. The spray-drying technique and process conditions selected were effective in microencapsulating and stabilizing the flavonoids content giving satisfactory encapsulation efficiency, product yield, morphology and enteric release.. Conclusion: This approach might be suitable for delivering natural bioactive extract such as Citrus Aurantium, avoiding gastric degradation of the molecule and improving its bioavailability from solid oral dosage forms.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11386/4629657
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