12th International Conference of Pharmaceutical Sciences

Hot-melt extrusion (HME) is a well-recognized technique to produce solid dispersions. Additionally, HME is becoming increasingly investigated for developing innovative drug delivery systems (Silva et al., 2018). To the best of our knowledge there are no reports on the use of HME for the preparation of proliposomes. In the present study, a film-casting technique was applied to investigate the miscibility between the model drug (lopinavir), polymers, plasticizers and lipids. Formulations containing soluplus or copovidone, soy lecithin, PEG400 and sodium taurodeoxycholate were selected and submitted to HME process using a vertical twin-screw mini-extruder. The resulting extrudates allow for a rapid liposome formation upon dilution in purified water. Size evaluation by dynamic light scattering showed a more homogeneous size distribution when soluplus-based extrudates were evaluated. HPLC analysis suggested the maintenance of lopinavir chemical stability during HME. The entrapment efficiency was superior to 90% for all tested formulations. These findings suggested that HME has great potential to prepare proliposomes.