The Impact of Various Poly(vinylpyrrolidone) Polymers on the Crystallization Process of Metronidazole.
Luiza OrszulakTaoufik LamraniMagdalena TarnackaBarbara HachułaKarolina JurkiewiczPatryk ZiołaAnna Mrozek-WilczkiewiczEwa KamińskaKamil KamińskiPublished in: Pharmaceutics (2024)
In this paper, we propose one-step synthetic strategies for obtaining well-defined linear and star-shaped polyvinylpyrrolidone ( lin PVP and star 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 ( w / w ), while the star-shaped polymer mixes with MTZ even at a 30:70 w / w . 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 w / w 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- star PVP 30:70 w / w system (which is not achievable for linear PVPs) demonstrated its complete amorphousness for over one month.