Preformulation study for the selection of a suitable polymer for the development of ellagic acid-based solid dispersion using hot-melt extrusion

Nyamba, Isaïe; Jennotte, Olivier; Sombié, Charles Bavouma; Lechanteur, Anna; Sacré, Pierre-Yves; Djandé, Abdoulaye; Semdé, Rasmané; Évrard, Brigitte

doi:10.1016/j.ijpharm.2023.123088

Cited by 7 publications

(1 citation statement)

References 79 publications

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“…The extrudates were browning in color with cellulosic polymer HPMC, which might be due to the charring of the polymer. LaFountaine et al prepared HPMC-based extrudates and found a similar brown color appearance [41], which is concomitant with the present experimental observations.…”

Section: Effect Of Polymer Type On Appearance Of Extrudates and Proce...supporting

confidence: 90%

QbD-Based Development and Evaluation of Pazopanib Hydrochloride Extrudates Prepared by Hot-Melt Extrusion Technique: In Vitro and In Vivo Evaluation

Gupta,

Dahima,

Panda

et al. 2024

Pharmaceutics

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Background: Pazopanib hydrochloride (PZB) is a protein kinase inhibitor approved by the United States Food and Drug Administration and European agencies for the treatment of renal cell carcinoma and other renal malignancies. However, it exhibits poor aqueous solubility and inconsistent oral drug absorption. In this regard, the current research work entails the development and evaluation of the extrudates of pazopanib hydrochloride by the hot-melt extrusion (HME) technique for solubility enhancement and augmenting oral bioavailability. Results: Solid dispersion of the drug was prepared using polymers such as Kollidon VA64, hydroxypropylmethylcellulose (HPMC), Eudragit EPO, and Affinisol 15LV in a 1:2 ratio by the HME process through a lab-scale 18 mm extruder. Systematic optimization of the formulation variables was carried out with the help of custom screening design (JMP Software by SAS, Version 14.0) to study the impact of polymer type and plasticizer level on the quality of extrudate processability by measuring the torque value, appearance, and disintegration time as the responses. The polymer blends containing Kollidon VA64 and Affinisol 15LV resulted in respective clear transparent extrudates, while Eudragit EPO and HPMC extrudates were found to be opaque white and brownish, respectively. Furthermore, evaluation of the impact of process parameters such as screw rpm and barrel temperature was measured using a definitive screening design on the extrude appearance, torque, disintegration time, and dissolution profile. Based on the statistical outcomes, it can be concluded that barrel temperature has a significant impact on torque, disintegration time, and dissolution at 30 min, while screw speed has an insignificant impact on the response variables. Affinisol extrudates showed less moisture uptake and faster dissolution in comparison to Kollidon VA64 extrudates. Affinisol extrudates were evaluated for polymorphic stability up to a 3-month accelerated condition and found no recrystallization. PZB–Extrudates using the Affinisol polymer (Test formulation A) revealed significantly higher bioavailability (AUC) in comparison to the free Pazopanib drug and marketed formulation.

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Section: Effect Of Polymer Type On Appearance Of Extrudates and Proce...supporting

confidence: 90%

QbD-Based Development and Evaluation of Pazopanib Hydrochloride Extrudates Prepared by Hot-Melt Extrusion Technique: In Vitro and In Vivo Evaluation

Gupta,

Dahima,

Panda

et al. 2024

Pharmaceutics

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Robust polymer hybrid and assembly materials from structure tailoring to efficient catalytic remediation of emerging pollutants

Ali,

Khan,

song

et al. 2024

Chemosphere

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Effects of hypromellose acetate succinate on recrystallization inhibition, miscibility, and dissolution enhancement of baloxavir marboxil solid dispersions

Wang,

Wu,

Wang

et al. 2024

International Journal of Biological Macromolecules

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Preformulation study for the selection of a suitable polymer for the development of ellagic acid-based solid dispersion using hot-melt extrusion

Cited by 7 publications

References 79 publications

QbD-Based Development and Evaluation of Pazopanib Hydrochloride Extrudates Prepared by Hot-Melt Extrusion Technique: In Vitro and In Vivo Evaluation

QbD-Based Development and Evaluation of Pazopanib Hydrochloride Extrudates Prepared by Hot-Melt Extrusion Technique: In Vitro and In Vivo Evaluation

Robust polymer hybrid and assembly materials from structure tailoring to efficient catalytic remediation of emerging pollutants

Effects of hypromellose acetate succinate on recrystallization inhibition, miscibility, and dissolution enhancement of baloxavir marboxil solid dispersions

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