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Saerens, L., Ghanam, D., Raemdonck, C., Francois, K., Manz, J., Krüger, R., Krüger, S., Vervaet, C., Remon, J.P. and De Beer, T. (2014) In-Line Solid State Prediction during Pharmaceutical Hot-Melt Extrusion in a 12mm Twin Screw Extruder Using Raman Spectroscopy. European Journal of Pharmaceutics and Biopharmaceutics, 87, 606-615.
https://doi.org/10.1016/j.ejpb.2014.03.002

has been cited by the following article:

• TITLE: Evaluating the Effects of Crystallinity on Drug Release Behaviour in Itraconazole- or Miconazole-Loaded PLGA Microparticles Prepared Using a Co-Grinding Method

  AUTHORS: Kazuhiro Matsuura, Honami Kojima, Miyako Yoshida, Takahiro Uchida

  KEYWORDS: Co-Grinding Method, Ball Milling, Poly (Lactide-co-Glycolide), Itraconazole, Miconazole, Amorphization

  JOURNAL NAME: Pharmacology & Pharmacy, Vol.14 No.9, September 8, 2023

  ABSTRACT: This study aimed to prepare and characterize itraconazole (ITCZ)- or miconazole (MCZ)-loaded poly (lactide-co-glycolide) (PLGA) microparticles (MP) using a co-grinding method with ball milling, which is a solvent-free and convenient procedure. PLGA MP was prepared by grinding for 60 min, and the fixed theoretical drug loading was set at 9.1% and 16.7% for both drugs. The obtained loading efficiency for both drugs was estimated to be approximately 100%. The average diameters of the drug-loaded PLGA MP were approximately 20 - 35 μm. Powder X-ray diffraction (PXRD) or differential scanning calorimetry (DSC) confirmed amorphization of ITCZ and MCZ in ITCZ- or MCZ-loaded PLGA MP in all formulations. The drug release percentage from 9.1%-loaded ITCZ-PLGA7505 MP at 24 h was almost 50%, which was higher than that of ITCZ powder. The drug release percentage from MCZ-loaded PLGA7505 MP at 4 h was over 80%, which was higher than that of MCZ powder. This enhancement of release rate is caused by the amorphization of ITCZ or MCZ in the PLGA matrix. MCZ-loaded PLGA7510 MP showed a sustained release profile up to 24 h, suggesting that MCZ exists in an amorphous form in the PLGA matrix; however, the release rate declined owing to the large molecular weight of PLGA. Therefore, the release enhancement of antifungal drugs loaded on PLGA MP could be achieved by their amorphization using a co-grinding method with ball milling.