20.500.12556/RUL-164728 The comparison of melt technologies based on mesoporous carriers for improved carvedilol dissolution High-shear (HS) melt granulation and hot melt extrusion (HME) were compared as perspective melt-based technologies for preparation of amorphous solid dispersions (ASDs). ASDs were prepared using mesoporous carriers (Syloid$^®$ 244FP or Neusilin$^®$ US2), which were loaded with carvedilol dispersed in polymeric matrix (polyethylene glycol 6000 or Soluplus$^®$). Formulations with high carvedilol content were obtained either by HME (11 extrudates with polymer:carrier ratio 1:1) or HS granulation (6 granulates with polymer:carrier ratio 3:1). DSC and XRD analysis confirmed the absence of crystalline carvedilol for the majority of prepared ADSs, thus confirming the stabilizing effect of selected polymers and carriers over amorphous carvedilol. HME produced larger particles compared to HS melt granulation, which was in line with better flow time and Carr index of extrudates. Moreover, SEM images revealed smoother surface of ASDs obtained by HME, contributing to less obstructed flow. The rougher and more porous surface of HS granules was correlated to larger granule specific surface area, manifesting in faster carvedilol release from Syloid$^®$ 244FP-based granules, as compared to their HME counterparts. Regarding dissolution, the two HS-formulations performed superior to pure crystalline carvedilol, thereby confirming the suitability of HS melt granulation for developing dosage forms with improved carvedilol dissolution. mesoporous carrier melt granulation hot melt extrusion PEG 6000 amorphous solid dispersion Soluplus$^Ⓡ$ mezoporozni nosilec granulacija taline ekstruzija vroče taline PEG 6000 amorfna trdna disperzija Soluplus$^Ⓡ$ farmacevtska tehnologija farmacevtske oblike true false true Angleški jezik Slovenski jezik Članek v reviji 2024-11-08 09:38:37 2024-11-08 09:38:40 2025-06-04 13:43:21 0000-00-00 00:00:00 2024 0 0 13 str. art. 106880 Vol. 202 2024 0000-00-00 Zaloznikova Objavljeno NiDoloceno 0000-00-00 0000-00-00 0000-00-00 661.12 0928-0987 10.1016/j.ejps.2024.106880 205524483 1-s2.0-S0928098724001921-main.pdf 1-s2.0-S0928098724001921-main.pdf 1 C362AF42E8D634F413AD690364CA17A5 542a7fecbd9f838de200f46ae6791fc5e542106ebc6ff7a24681be76c253e480 154391f4-9dad-11ef-b232-0050569b8976 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=195356 https://www.sciencedirect.com/science/article/pii/S0928098724001921 1 81ba4394-9dac-11ef-b232-0050569b8976 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=195355 Fakulteta za farmacijo 0 0 0