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Preparation of floating polymer-valsartan delivery systems using supercritical CO2

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Abstract

This study investigates pharmaceutical polymers (Soluplus®, HPMCAS, and Eudragit® E100) and supercritical CO2-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/m3. 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.

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Abbreviations

EUD:

Eudragit® E100

HPMCAS:

Hydroxypropyl methylcellulose acetate succinate

PBS:

Phosphate buffer solution

ScCO2:

Supercritical carbon dioxide

SOL:

Soluplus®

VAL:

Valsartan

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Acknowledgment

This work was supported by the Ministry of Education, Science and Technological Development of the Republic of Serbia (Contract No. 451-03-68/2020-14/200135). Authors thank Hemofarm (Vršac, Serbia) for providing Hydroxypropyl methylcellulose acetate succinate (HPMCAS) and Valsartan. Authors thank Dr. Miroslav Stankovic from Institute of Chemistry, Technology and Metallurgy (University of Belgrade) for assistance in mercury porosimetry measurements.

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Authors and Affiliations

  1. Faculty of Technology and Metallurgy, University of Belgrade, Karnegijeva 4, 11120, Belgrade, Serbia

    Stoja Milovanovic & Aleksandra Dapčević

  2. Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221, Belgrade, Serbia

    Jelena Djuris, Djordje Medarevic & Svetlana Ibric

  3. Innovation Center of the Faculty of Technology and Metallurgy, University of Belgrade, Karnegijeva 4, 11120 Belgrade, Serbia

    Marija Lucic Skoric

  4. Institute of Chemistry, Technology and Metallurgy, University of Belgrade, Njegoševa 12, 11000, Belgrade, Serbia

    Stefan M. Pavlović

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  1. Stoja Milovanovic
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  2. Jelena Djuris
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  3. Aleksandra Dapčević
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  4. Marija Lucic Skoric
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  5. Djordje Medarevic
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  6. Stefan M. Pavlović
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  7. Svetlana Ibric
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Correspondence to Stoja Milovanovic.

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Milovanovic, S., Djuris, J., Dapčević, A. et al. Preparation of floating polymer-valsartan delivery systems using supercritical CO2. J Polym Res 28, 74 (2021). https://doi.org/10.1007/s10965-021-02440-1

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