Preparation of floating polymer-valsartan delivery systems using supercritical CO2

• Published in: Journal of polymer research Vol. 28; no. 3
• Main Authors: Milovanovic, Stoja, Djuris, Jelena, Dapčević, Aleksandra, Skoric, Marija Lucic, Medarevic, Djordje, Pavlović, Stefan M., Ibric, Svetlana
• Format: Journal Article
• Language: English
• Published: Dordrecht Springer Netherlands 2021; Springer Nature B.V
• Subjects: Bulk density; Buoyancy; Carbon dioxide; Characterization and Evaluation of Materials; Chemistry; Chemistry and Materials Science; Drug delivery systems; Industrial Chemistry/Chemical Engineering; Original Paper; Polymer Sciences; Polymers; Porosity; HPMCAS; Soluplus; Valsartan; E100; Eudragit; Supercritical CO
• ISSN: 1022-9760; 1572-8935
• DOI: 10.1007/s10965-021-02440-1

This study investigates pharmaceutical polymers (Soluplus ® , HPMCAS, and Eudragit ® E100) and supercritical CO 2 -assisted process for preparation of floating valsartan delivery systems. Tested process (at pressure of 30 MPa and temperature of 100 °C during 2 h) enabled preparation of stable porous valsartan formulations which was confirmed with FESEM and mercury intrusion porosimetry analysis. The bulk density of obtained formulations was lower than 550 kg/m 3 . FTIR, DSC, and PXRD analysis indicated that there was no chemical interaction between the drug and polymers and that amorphous solid dispersions were obtained. Formulations with Soluplus ® and HPMCAS retained its buoyancy in 0.1 M HCl for longer than 24 h, while formulation with Eudragit ® E100 retained its buoyancy up to 2 h. Controlled valsartan release was influenced by solubility of polymers in the tested release medium, which was confirmed by UV/VIS spectroscopy. The obtained results provided framework for further development of floating drug delivery system using an environmental friendly process.