In this paper, we propose one-step synthetic strategies for obtaining well-defined linear and star-shaped polyvinylpyrrolidone (PVP and PVP). The produced macromolecules and a commercial PVP K30 with linear topology were investigated as potential matrices for suppressing metronidazole (MTZ) crystallization. Interestingly, during the formation of binary mixtures (BMs) containing different polymers and MTZ, we found that linear PVPs exhibit maximum miscibility with the drug at a 50:50 weight ratio (/), while the star-shaped polymer mixes with MTZ even at a 30:70 /. To explain these observations, comprehensive studies of MTZ-PVP formulations with various contents of both components were performed using Fourier-transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction. The obtained results clearly showed that the polymer's topology plays a significant role in the type of interactions occurring between the matrix and MTZ. Additionally, we established that for MTZ-PVP 50:50 and 75:25 / BMs, linear polymers have the most substantial impact on inhibiting the crystallization of API. The star-shaped macromolecule turned out to be the least effective in stabilizing amorphous MTZ at these polymer concentrations. Nevertheless, long-term structural investigations of the MTZ-PVP 30:70 / system (which is not achievable for linear PVPs) demonstrated its complete amorphousness for over one month.
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| http://dx.doi.org/10.3390/pharmaceutics16010136 | DOI Listing |
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Article Synopsis
- This study examines how the molecular weight of polyvinylpyrrolidone (PVP) affects the dissolution and effectiveness of celecoxib (CCX) when mixed into amorphous solid dispersions.
- It was found that lower molecular weight PVP increased the dissolution rate of CCX, while higher molecular weights provided better crystallization inhibition, peaking at PVP K30.
- Results showed that higher molecular weight PVP formulations led to better bioavailability of CCX in live organisms, suggesting the in vitro tests could accurately predict in vivo performance.
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