Abstract
High speed electrospinning (HSES), compatible with pharmaceutical industry, was used to demonstrate the viability of the preparation of drug-loaded polymer nanofibers with radically higher productivity than the known single-needle electrospinning (SNES) setup. Poorly water-soluble itraconazole (ITRA) was formulated with PVPVA64 matrix polymer using four different solvent-based methods such as HSES, SNES, spray drying (SD)and film casting (FC). The formulations were assessed in terms of improvement in the dissolution rate of ITRA (using a "tapped basket" dissolution configuration) and analysed by SEM, DSC and XRPD. Despite the significantly increased productivity of HSES, the obtained morphology was very similar to the SNES nanofibrous material. ITRA transformed into an amorphous form, according to the DSC and XRPD results, in most cases except the FC samples. The limited dissolution of crystalline ITRA could be highly improved: fast dissolution occurred (>90% within 10 min) in the cases of both (the scaled-up and the single-needle) types of electrospun fibers, while the improvement in the dissolution rate of the spray-dried microspheres was significantly lower. Production of amorphous solid dispersions (ASDs) with the HSES system proved to be flexibly scalable and easy to integrate into a continuous pharmaceutical manufacturing line, which opens new routes for the development of industrially relevant nanopharmaceuticals.
| Original language | English |
|---|---|
| Pages (from-to) | 137-142 |
| Number of pages | 6 |
| Journal | International Journal of Pharmaceutics |
| Volume | 480 |
| Issue number | 1-2 |
| DOIs | |
| Publication status | Published - márc. 1 2015 |
Fingerprint
ASJC Scopus subject areas
- Pharmaceutical Science
Cite this
High speed electrospinning for scaled-up production of amorphous solid dispersion of itraconazole. / Nagy, Zsombor K.; Balogh, Attila; Démuth, Balázs; Pataki, Hajnalka; Vigh, Tamás; Szabó, Bence; Molnár, Kolos; Schmidt, Bence T.; Horák, Péter; Marosi, G.; Verreck, Geert; Van Assche, Ivo; Brewster, Marcus E.
In: International Journal of Pharmaceutics, Vol. 480, No. 1-2, 01.03.2015, p. 137-142.Research output: Article
}
TY - JOUR
T1 - High speed electrospinning for scaled-up production of amorphous solid dispersion of itraconazole
AU - Nagy, Zsombor K.
AU - Balogh, Attila
AU - Démuth, Balázs
AU - Pataki, Hajnalka
AU - Vigh, Tamás
AU - Szabó, Bence
AU - Molnár, Kolos
AU - Schmidt, Bence T.
AU - Horák, Péter
AU - Marosi, G.
AU - Verreck, Geert
AU - Van Assche, Ivo
AU - Brewster, Marcus E.
PY - 2015/3/1
Y1 - 2015/3/1
N2 - High speed electrospinning (HSES), compatible with pharmaceutical industry, was used to demonstrate the viability of the preparation of drug-loaded polymer nanofibers with radically higher productivity than the known single-needle electrospinning (SNES) setup. Poorly water-soluble itraconazole (ITRA) was formulated with PVPVA64 matrix polymer using four different solvent-based methods such as HSES, SNES, spray drying (SD)and film casting (FC). The formulations were assessed in terms of improvement in the dissolution rate of ITRA (using a "tapped basket" dissolution configuration) and analysed by SEM, DSC and XRPD. Despite the significantly increased productivity of HSES, the obtained morphology was very similar to the SNES nanofibrous material. ITRA transformed into an amorphous form, according to the DSC and XRPD results, in most cases except the FC samples. The limited dissolution of crystalline ITRA could be highly improved: fast dissolution occurred (>90% within 10 min) in the cases of both (the scaled-up and the single-needle) types of electrospun fibers, while the improvement in the dissolution rate of the spray-dried microspheres was significantly lower. Production of amorphous solid dispersions (ASDs) with the HSES system proved to be flexibly scalable and easy to integrate into a continuous pharmaceutical manufacturing line, which opens new routes for the development of industrially relevant nanopharmaceuticals.
AB - High speed electrospinning (HSES), compatible with pharmaceutical industry, was used to demonstrate the viability of the preparation of drug-loaded polymer nanofibers with radically higher productivity than the known single-needle electrospinning (SNES) setup. Poorly water-soluble itraconazole (ITRA) was formulated with PVPVA64 matrix polymer using four different solvent-based methods such as HSES, SNES, spray drying (SD)and film casting (FC). The formulations were assessed in terms of improvement in the dissolution rate of ITRA (using a "tapped basket" dissolution configuration) and analysed by SEM, DSC and XRPD. Despite the significantly increased productivity of HSES, the obtained morphology was very similar to the SNES nanofibrous material. ITRA transformed into an amorphous form, according to the DSC and XRPD results, in most cases except the FC samples. The limited dissolution of crystalline ITRA could be highly improved: fast dissolution occurred (>90% within 10 min) in the cases of both (the scaled-up and the single-needle) types of electrospun fibers, while the improvement in the dissolution rate of the spray-dried microspheres was significantly lower. Production of amorphous solid dispersions (ASDs) with the HSES system proved to be flexibly scalable and easy to integrate into a continuous pharmaceutical manufacturing line, which opens new routes for the development of industrially relevant nanopharmaceuticals.
KW - Amorphous solid dispersion
KW - Continuous nanoformulation
KW - Dissolution enhancement
KW - Electrospinning
KW - Itraconazole
KW - Scaling-up
UR - http://www.scopus.com/inward/record.url?scp=84921730384&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84921730384&partnerID=8YFLogxK
U2 - 10.1016/j.ijpharm.2015.01.025
DO - 10.1016/j.ijpharm.2015.01.025
M3 - Article
C2 - 25596415
AN - SCOPUS:84921730384
VL - 480
SP - 137
EP - 142
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
SN - 0378-5173
IS - 1-2
ER -