TY - JOUR
T1 - SEDEX—Self-Emulsifying Delivery Via Hot Melt Extrusion
T2 - A Continuous Pilot-Scale Feasibility Study
AU - Zupančič, Ožbej
AU - Doğan, Aygün
AU - Matić, Josip
AU - Kushwah, Varun
AU - Alva, Carolina
AU - Spoerk, Martin
AU - Paudel, Amrit
N1 - Funding Information:
This work was funded through the Austria COMET Program by the Austrian Federal Ministry of Climate Action, Environment, Energy, Mobility, Innovation, and Technology; the Austrian Federal Ministry of Labor and Economy, the Federal State of Styria and SFG. The COMET Program is managed by the Austrian FFG.
Publisher Copyright:
© 2022 by the authors.
PY - 2022/12
Y1 - 2022/12
N2 - The aim of this study was to develop a continuous pilot-scale solidification and characterization of self-emulsifying drug delivery systems (SEDDSs) via hot melt extrusion (HME) using Soluplus® and Kollidon® VA-64. First, an oil-binding capacity study was performed to estimate the maximal amount of SEDDSs that the polymers could bind. Then, HME was conducted using a Coperion 18 mm ZSK18 pilot plant-scale extruder with split-feeding of polymer and SEDDS in 10, 20, and 30% w/w SEDDSs was conducted. The prepared extrudates were characterized depending on appearance, differential scanning calorimetry, wide-angle X-ray scattering, emulsification time, droplet size, polydispersity index, and cloud point. The oil-binding studies showed that the polymers were able to bind up to 50% w/w of liquid SEDDSs. The polymers were processed via HME in a temperature range between 110 and 160 °C, where a plasticizing effect of the SEDDSs was observed. The extrudates were found to be stable in the amorphous state and self-emulsified in demineralized water at 37 °C with mean droplet sizes between 50 and 300 nm. A cloud point and phase inversion were evident in the Soluplus® samples. In conclusion, processing SEDDSs with HME could be considered a promising alternative to the established solidification techniques as well as classic amorphous solid dispersions for drug delivery.
AB - The aim of this study was to develop a continuous pilot-scale solidification and characterization of self-emulsifying drug delivery systems (SEDDSs) via hot melt extrusion (HME) using Soluplus® and Kollidon® VA-64. First, an oil-binding capacity study was performed to estimate the maximal amount of SEDDSs that the polymers could bind. Then, HME was conducted using a Coperion 18 mm ZSK18 pilot plant-scale extruder with split-feeding of polymer and SEDDS in 10, 20, and 30% w/w SEDDSs was conducted. The prepared extrudates were characterized depending on appearance, differential scanning calorimetry, wide-angle X-ray scattering, emulsification time, droplet size, polydispersity index, and cloud point. The oil-binding studies showed that the polymers were able to bind up to 50% w/w of liquid SEDDSs. The polymers were processed via HME in a temperature range between 110 and 160 °C, where a plasticizing effect of the SEDDSs was observed. The extrudates were found to be stable in the amorphous state and self-emulsified in demineralized water at 37 °C with mean droplet sizes between 50 and 300 nm. A cloud point and phase inversion were evident in the Soluplus® samples. In conclusion, processing SEDDSs with HME could be considered a promising alternative to the established solidification techniques as well as classic amorphous solid dispersions for drug delivery.
KW - hot melt extrusion (HME)
KW - pilot scale production
KW - SEDDSs characterization
KW - self-emulsifying drug delivery systems (SEDDSs)
KW - solid SEDDSs
KW - ZSK18
UR - http://www.scopus.com/inward/record.url?scp=85144678294&partnerID=8YFLogxK
U2 - 10.3390/pharmaceutics14122617
DO - 10.3390/pharmaceutics14122617
M3 - Article
AN - SCOPUS:85144678294
SN - 1999-4923
VL - 14
JO - Pharmaceutics
JF - Pharmaceutics
IS - 12
M1 - 2617
ER -