The effect of the molecular weight of polyvinylpyrrolidone and the model drug on laser-induced in situ amorphization
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The effect of the molecular weight of polyvinylpyrrolidone and the model drug on laser-induced in situ amorphization. / Hempel, Nele Johanna; Merkl, Padryk; Knopp, Matthias Manne; Berthelsen, Ragna; Teleki, Alexandra; Hansen, Anders Kragh; Sotiriou, Georgios A.; Löbmann, Korbinian.
In: Molecules, Vol. 26, No. 13, 4035, 07.2021.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - The effect of the molecular weight of polyvinylpyrrolidone and the model drug on laser-induced in situ amorphization
AU - Hempel, Nele Johanna
AU - Merkl, Padryk
AU - Knopp, Matthias Manne
AU - Berthelsen, Ragna
AU - Teleki, Alexandra
AU - Hansen, Anders Kragh
AU - Sotiriou, Georgios A.
AU - Löbmann, Korbinian
N1 - This article belongs to the Collection Poorly Soluble Drugs.
PY - 2021/7
Y1 - 2021/7
N2 - 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.
AB - 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.
KW - Amorphous solid dispersion
KW - Dissolution kinetics
KW - In situ amorphization
KW - Near-IR laser radiation
KW - Plasmonic photothermal nanoparticles
U2 - 10.3390/molecules26134035
DO - 10.3390/molecules26134035
M3 - Journal article
C2 - 34279377
AN - SCOPUS:85109906003
VL - 26
JO - Molecules (Print Archive Edition)
JF - Molecules (Print Archive Edition)
SN - 1431-5157
IS - 13
M1 - 4035
ER -
ID: 279121380