期刊
MOLECULES
卷 26, 期 13, 页码 -出版社
MDPI
DOI: 10.3390/molecules26134035
关键词
in situ amorphization; near-IR laser radiation; amorphous solid dispersion; plasmonic photothermal nanoparticles; dissolution kinetics
资金
- NordForsk (Nordic University Hub) [85352]
- Independent Research Fund Denmark [DFF-7026-00052B]
- European Research Council (ERC) under the European Union [758705]
- Swedish Foundation for Strategic Research [FFL18-0043]
- Swedish Research Council [2016-03471]
- Science for Life Laboratory
- European Research Council (ERC) [758705] Funding Source: European Research Council (ERC)
- Swedish Foundation for Strategic Research (SSF) [FFL18-0043] Funding Source: Swedish Foundation for Strategic Research (SSF)
- Swedish Research Council [2016-03471] Funding Source: Swedish Research Council
Laser radiation has been used to achieve in situ drug amorphization, with the study showing that the molecular weight of the polymer and the properties of the drug have a significant impact on dissolution kinetics. Lower molecular weight PVP12 showed faster amorphization rates compared to PVP17 and PVP25, with naproxen demonstrating the fastest rate among the three drugs studied.
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 (T-g) 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 (M-w) 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 M-w of polyvinylpyrrolidone (PVP: PVP12, PVP17 or PVP25), 0.25 wt% plasmonic nanoaggregates (PNs) and 0.5 wt% lubricant, the effect of the polymer M-w 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 M-w (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.
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