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

Autor: Anders Kragh Hansen, Ragna Berthelsen, Matthias Manne Knopp, Nele Johanna Hempel, Georgios A. Sotiriou, Alexandra Teleki, Korbinian Löbmann, Padryk Merkl
Rok vydání: 2021
Předmět:
Naproxen
Materials science
Infrared Rays
Pharmaceutical Science
02 engineering and technology
030226 pharmacology & pharmacy
Article
Dosage form
Analytical Chemistry
Pharmaceutical Sciences
03 medical and health sciences
QD241-441
0302 clinical medicine
amorphous solid dispersion
Drug Stability
Drug Discovery
medicine
Physical and Theoretical Chemistry
Solubility
Dissolution
chemistry.chemical_classification
Polyvinylpyrrolidone
Viscosity
in situ amorphization
Lasers
Organic Chemistry
Anti-Inflammatory Agents
Non-Steroidal

near-IR laser radiation
Povidone
Polymer
Farmaceutiska vetenskaper
021001 nanoscience & nanotechnology
plasmonic photothermal nanoparticles
chemistry
Chemistry (miscellaneous)
Celecoxib
Molecular Medicine
Nanoparticles
Particle size
0210 nano-technology
Glass transition
dissolution kinetics
medicine.drug
Nuclear chemistry
Zdroj: Molecules
Volume 26
Issue 13
Hempel, N J, Merkl, P, Knopp, M M, Berthelsen, R, Teleki, A, Hansen, A K, Sotiriou, G A & Löbmann, K 2021, ' The effect of the molecular weight of polyvinylpyrrolidone and the model drug on laser-induced in situ amorphization ', Molecules, vol. 26, no. 13, 4035 . https://doi.org/10.3390/molecules26134035
Molecules, Vol 26, Iss 4035, p 4035 (2021)
ISSN: 1420-3049
Popis: 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.
Databáze: OpenAIRE
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