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Article

The Effect of the Molecular Weight of Polyvinylpyrrolidone and the Model Drug on Laser-Induced In Situ Amorphization

1
Department of Pharmacy, University of Copenhagen, 2100 Copenhagen, Denmark
2
Department of Microbiology, Tumor and Cell Biology, Karolinska Institute, 17177 Stockholm, Sweden
3
Bioneer:FARMA, Department of Pharmacy, University of Copenhagen, 2100 Copenhagen, Denmark
4
Science for Life Laboratory, Department of Pharmacy, Uppsala University, 75123 Uppsala, Sweden
5
Department of Photonics Engineering, Technical University of Denmark, 4000 Roskilde, Denmark
*
Author to whom correspondence should be addressed.
Academic Editor: Josef Jampilek
Molecules 2021, 26(13), 4035; https://doi.org/10.3390/molecules26134035
Received: 10 June 2021 / Revised: 25 June 2021 / Accepted: 25 June 2021 / Published: 1 July 2021
(This article belongs to the Collection Poorly Soluble Drugs)
Laser radiation has been shown to be a promising approach for in situ amorphization, i.e., drug amorphization inside the final dosage form. Upon exposure to laser radiation, elevated temperatures in the compacts are obtained. At temperatures above the glass transition temperature (Tg) of the polymer, the drug dissolves into the mobile polymer. Hence, the dissolution kinetics are dependent on the viscosity of the polymer, indirectly determined by the molecular weight (Mw) of the polymer, the solubility of the drug in the polymer, the particle size of the drug and the molecular size of the drug. Using compacts containing 30 wt% of the drug celecoxib (CCX), 69.25 wt% of three different Mw of polyvinylpyrrolidone (PVP: PVP12, PVP17 or PVP25), 0.25 wt% plasmonic nanoaggregates (PNs) and 0.5 wt% lubricant, the effect of the polymer Mw on the dissolution kinetics upon exposure to laser radiation was investigated. Furthermore, the effect of the model drug on the dissolution kinetics was investigated using compacts containing 30 wt% of three different drugs (CCX, indomethacin (IND) and naproxen (NAP)), 69.25 wt% PVP12, 0.25 wt% PN and 0.5 wt% lubricant. In perfect correlation to the Noyes–Whitney equation, this study showed that the use of PVP with the lowest viscosity, i.e., the lowest Mw (here PVP12), led to the fastest rate of amorphization compared to PVP17 and PVP25. Furthermore, NAP showed the fastest rate of amorphization, followed by IND and CCX in PVP12 due to its high solubility and small molecular size. View Full-Text
Keywords: in situ amorphization; near-IR laser radiation; amorphous solid dispersion; plasmonic photothermal nanoparticles; dissolution kinetics in situ amorphization; near-IR laser radiation; amorphous solid dispersion; plasmonic photothermal nanoparticles; dissolution kinetics
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MDPI and ACS Style

Hempel, N.-J.; Merkl, P.; Knopp, M.M.; Berthelsen, R.; Teleki, A.; Hansen, A.K.; Sotiriou, G.A.; Löbmann, K. The Effect of the Molecular Weight of Polyvinylpyrrolidone and the Model Drug on Laser-Induced In Situ Amorphization. Molecules 2021, 26, 4035. https://doi.org/10.3390/molecules26134035

AMA Style

Hempel N-J, Merkl P, Knopp MM, Berthelsen R, Teleki A, Hansen AK, Sotiriou GA, Löbmann K. The Effect of the Molecular Weight of Polyvinylpyrrolidone and the Model Drug on Laser-Induced In Situ Amorphization. Molecules. 2021; 26(13):4035. https://doi.org/10.3390/molecules26134035

Chicago/Turabian Style

Hempel, Nele-Johanna, Padryk Merkl, Matthias M. Knopp, Ragna Berthelsen, Alexandra Teleki, Anders K. Hansen, Georgios A. Sotiriou, and Korbinian Löbmann. 2021. "The Effect of the Molecular Weight of Polyvinylpyrrolidone and the Model Drug on Laser-Induced In Situ Amorphization" Molecules 26, no. 13: 4035. https://doi.org/10.3390/molecules26134035

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