Water Sorption in Glassy Polyvinylpyrrolidone-Based Polymers

Borrmann, Dominik; Danzer, Andreas; Sadowski, Gabriele

doi:10.3390/membranes12040434

Cited by 16 publications

(33 citation statements)

References 47 publications

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“…The PVP-IND solutions contained 58 wt% ethanol for both drug loads and were spun at 2000 rpm for the drug load of 0.2 and at 1150 rpm for a drug load of 0.5. These specifications allowed the preparation of ASD films with thicknesses of ~7-9 µm, making them comparable to the PVP and PVPVA films and the amorphous IND films from our previous works [9,10]. Furthermore, the geometry of all considered films represents an ideal cylinder, and all films share the same circular base area with a diameter of 14.5 mm.…”

Section: Film Preparationmentioning

confidence: 99%

“…We applied a spin-coating technique described in our previous study [9] to prepare PVP-IND and PVPVA-IND ASD films. A circular glass coverslip (18 mm in diameter) was masked with a perforated polystyrene foil and then coated with an ethanolic polymer-API solution using a spin-coating device (Süss MicroTec D80T2 spin coater).…”

Section: Film Preparationmentioning

confidence: 99%

“…However, substantial deviations occur when modelling the volume of glassy mixtures. The NET-GP approach was used together with PC-SAFT providing an accurate representation of the pressure-volume-temperature behavior of a glassy polymer [9]. We applied the transition rule for the fugacity of water f L w displayed in Equation ( 6) derived in our previous work [9].…”

Section: Calculations Of Water-sorption Isothermsmentioning

confidence: 99%

“…The PC-SAFT modeling with NET-GP switches to PC-SAFT modeling without NET-GP when the equilibrium mole fraction x EQ w of water becomes greater than the non-equilibrium mole fraction x NE w of water. PC-SAFT modeling without NET-GP requires the volume V EQ of the ASD-water mixture in equilibrium at the system's temperature T and pressure p. In contrast, PC-SAFT modeling with NET-GP requires the volume V NE of the ASD-water mixture in non-equilibrium given by Equation ( 7) as a function of the relative humidity RH as used in previous work [9].…”

Section: Calculations Of Water-sorption Isothermsmentioning

confidence: 99%

“…The NET-GP approach for polymer blends, as proposed by Sarti and Dogheri [15], suggests a volumetric mixing rule for k NE w . Hence, the swelling coefficient k NE w of the ASD by water was described according to Equation (9).…”

Section: Calculations Of Water-sorption Isothermsmentioning

confidence: 99%

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Predicting the Water Sorption in ASDs

2022

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Water decreases the stability of amorphous solid dispersions (ASDs) and water sorption is, therefore, unwanted during ASD storage. This work suggests a methodology to predict the water-sorption isotherms and the water-sorption kinetics in amorphous pharmaceutical formulations like ASDs. We verified the validity of the proposed methodology by measuring and predicting the water-sorption curves in ASD films of polyvinylpyrrolidone-based polymers and of indomethacin. This way, the extent and the rate of water sorption in ASDs were predicted for drug loads of 0.2 and 0.5 as well as in the humidity range from 0 to 0.9 RH at 25 °C. The water-sorption isotherms and the water-sorption kinetics in the ASDs were predicted only based on the water-sorption isotherms and water-sorption kinetics in the neat polymer on the one hand and in the neat active pharmaceutical ingredient (API) on the other hand. The accurate prediction of water-sorption isotherms was ensured by combining the Perturbed-Chain Statistical Association Theory (PC-SAFT) with the Non-Equilibrium Thermodynamics of Glassy Polymers (NET-GP) approach. Water-sorption kinetics were predicted using Maxwell–Stefan diffusion coefficients of water in the ASDs.

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Section: Film Preparationmentioning

confidence: 99%

Section: Film Preparationmentioning

confidence: 99%

Section: Calculations Of Water-sorption Isothermsmentioning

confidence: 99%

Section: Calculations Of Water-sorption Isothermsmentioning

confidence: 99%

Section: Calculations Of Water-sorption Isothermsmentioning

confidence: 99%

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Predicting the Water Sorption in ASDs

2022

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Investigating the effect of polyvinylpyrrolidone matrix on surface characteristics and dissolution rate of anticancer drug dasatinib

Sokač,

Priselec,

Barač

et al. 2024

J of Applied Polymer Sci

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Dasatinib (DAS) is a second‐generation tyrosine kinase inhibitor used in the treatment of Philadelphia chromosome‐positive chronic myeloid leukemia and acute lymphoblastic leukemia. Nevertheless, this drug is hindered by poor gastrointestinal absorption and limited bioavailability, primarily attributable to its low aqueous solubility. To improve its properties, solid dispersions of DAS within a matrix of the hydrophilic polymer polyvinylpyrrolidone (PVP) are prepared by cogrinding in a vibrational ball mill at various drug‐to‐polymer ratios. The prepared solid dispersions are thoroughly characterized by several methods to verify the drug's amorphization and enhanced wettability as a result of successful mechanochemical activation. Fluidized bed melt granulation and traditional tableting are used to prepare tablets of 8 mm diameter with strictly defined aimed properties. Characterization of tablets includes testing their hardness, disintegration, and in vitro dissolution. The in vitro release profiles reveal a significant improvement in the release rate of DAS from tablets containing solid dispersion with the highest polymer ratio when compared with those containing untreated DAS or solid dispersions with a low polymer ratio. The results confirm the significant effect of the PVP ratio in solid dispersions on the surface characteristics and dissolution rate of DAS.

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