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Article

The Influence of Drug–Polymer Solubility on Laser-Induced In Situ Drug Amorphization Using Photothermal Plasmonic Nanoparticles

1
Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, Denmark
2
Department of Microbiology, Tumor and Cell Biology, Karolinska Institutet, 17177 Stockholm, Sweden
3
Department of Pharmacy, Bioneer:FARMA, 2100 Copenhagen, Denmark
4
Department of Pharmacy, Science for Life Laboratory, Uppsala University, 75123 Uppsala, Sweden
*
Author to whom correspondence should be addressed.
Academic Editor: Tomáš Etrych
Pharmaceutics 2021, 13(6), 917; https://doi.org/10.3390/pharmaceutics13060917
Received: 10 May 2021 / Revised: 17 June 2021 / Accepted: 18 June 2021 / Published: 21 June 2021
(This article belongs to the Special Issue Advances in Amorphous Drug Formulations, Volume II)
In this study, laser-induced in situ amorphization (i.e., amorphization inside the final dosage form) of the model drug celecoxib (CCX) with six different polymers was investigated. The drug–polymer combinations were studied with regard to the influence of (i) the physicochemical properties of the polymer, e.g., the glass transition temperature (Tg) and (ii) the drug–polymer solubility on the rate and degree of in situ drug amorphization. Compacts were prepared containing 30 wt% CCX, 69.25 wt% polymer, 0.5 wt% lubricant, and 0.25 wt% plasmonic nanoparticles (PNs) and exposed to near-infrared laser radiation. Upon exposure to laser radiation, the PNs generated heat, which allowed drug dissolution into the polymer at temperatures above its Tg, yielding an amorphous solid dispersion. It was found that in situ drug amorphization was possible for drug–polymer combinations, where the temperature reached during exposure to laser radiation was above the onset temperature for a dissolution process of the drug into the polymer, i.e., TDStart. The findings of this study showed that the concept of laser-induced in situ drug amorphization is applicable to a range of polymers if the drug is soluble in the polymer and temperatures during the process are above TDStart. View Full-Text
Keywords: oral drug delivery; in situ drug amorphization; polymers; amorphous solid dispersion; laser radiation; plasmonic nanoparticles; pharmaceutical nanotechnology oral drug delivery; in situ drug amorphization; polymers; amorphous solid dispersion; laser radiation; plasmonic nanoparticles; pharmaceutical nanotechnology
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MDPI and ACS Style

Hempel, N.-J.; Merkl, P.; Knopp, M.M.; Berthelsen, R.; Teleki, A.; Sotiriou, G.A.; Löbmann, K. The Influence of Drug–Polymer Solubility on Laser-Induced In Situ Drug Amorphization Using Photothermal Plasmonic Nanoparticles. Pharmaceutics 2021, 13, 917. https://doi.org/10.3390/pharmaceutics13060917

AMA Style

Hempel N-J, Merkl P, Knopp MM, Berthelsen R, Teleki A, Sotiriou GA, Löbmann K. The Influence of Drug–Polymer Solubility on Laser-Induced In Situ Drug Amorphization Using Photothermal Plasmonic Nanoparticles. Pharmaceutics. 2021; 13(6):917. https://doi.org/10.3390/pharmaceutics13060917

Chicago/Turabian Style

Hempel, Nele-Johanna, Padryk Merkl, Matthias M. Knopp, Ragna Berthelsen, Alexandra Teleki, Georgios A. Sotiriou, and Korbinian Löbmann. 2021. "The Influence of Drug–Polymer Solubility on Laser-Induced In Situ Drug Amorphization Using Photothermal Plasmonic Nanoparticles" Pharmaceutics 13, no. 6: 917. https://doi.org/10.3390/pharmaceutics13060917

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