Záhonyi, Petra and Müncz, Áron Gábor and Péter-Haraszti, Anna and Nagy, Zsombor Kristóf and Csontos, István and Marosi, György and Szabó, Edina (2025) Continuous twin-screw melt granulation of drug-loaded electrospun fibers. EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 206. No. 114580. ISSN 0939-6411
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Abstract
Electrospinning (ES) is a promising continuous formulation strategy to produce amorphous solid dispersions (ASDs) and thereby improve the dissolution of poorly water-soluble drugs. However, processing the electrospun material into solid dosage forms (e.g. tablets) is challenging due to the poor flow properties. In this research, continuous twin-screw melt granulation was applied to improve the flowability of the fibers and therefore ease the further processing steps. During this work, two ASD compositions were investigated: one containing 60 % poly-vinylpyrrolidone-vinyl acetate 6:4 copolymer and 40 % itraconazole (ITR), and another one containing hydroxypropyl methylcellulose (HPMC) and ITR in the same ratio. Both fiber compositions were granulated with polyethene glycol as the binder material, while the effects of the process parameters were examined. The application of higher granulation temperature and screw configurations with increased shear forces compromised the fibrous structure, induced crystallization of the ASD, and decreased the dissolution. However, the stability of the ITR-HPMC fibers proved to be higher as their granulation at 60 °C led to granules with adequate flow properties and dissolution. Moreover, tablets with fewer excipients were pressed from them, resulting in a 34 % reduction in weight. Consequently, this process can complement ES technology and facilitate its industrial implementation. © 2024 The Authors
| Item Type: | Article |
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| Additional Information: | Correspondence Address: Szabó, E.; Department of Organic Chemistry and Technology, Műegyetem rkp. 3., Hungary; email: szabo.edina@vbk.bme.hu Chemicals/CAS: hydroxypropylmethylcellulose, 9004-65-3; itraconazole, 84625-61-6; macrogol, 25322-68-3; povidone, 9003-39-8; vinyl acetate, 108-05-4 Manufacturers: Sigma Aldrich, United States Funding details: European Commission, EC Funding details: Magyar Tudományos Akadémia, MTA Funding details: Nemzeti Kutatási, Fejlesztési és Innovaciós Alap, NKFIA Funding details: Nemzeti Kutatási Fejlesztési és Innovációs Hivatal, NKFIH, K 143039, ÚNKP-23-3-II-BME-242, ÚNKP-23-5-BME - 421 Funding details: Nemzeti Kutatási Fejlesztési és Innovációs Hivatal, NKFIH Funding text 1: Project no. RRF-2.3.1-21-2022-00015 has been implemented with the support provided by the European Union . This paper was supported by the J\\u00E1nos Bolyai Research Scholarship of the Hungarian Academy of Science. This research was supported from grants by National Research, Development and Innovation Office of Hungary (grant numbers: K 143039 ). This project was supported by the \\u00DANKP-23-3-II-BME-242 and \\u00DANKP-23-5-BME - 421 New National Excellence Program of the Ministry for Culture and Innovation from the source of the National Research, Development and Innovation Fund . The scientific research publicized in this article was reached with the sponsorship of Gedeon Richter Talentum Foundation in framework of Gedeon Richter Excellence PhD Scholarship of Gedeon Richter. The authors would like to thank Erzs\\u00E9bet T\\u00F3th for her help with the MDSC measurements. The authors would like to express their gratitude to Bal\\u00E1zs Pinke for his help with the SEM measurement, and Prof. Krisztina L\\u00E1szl\\u00F3 and Anna Bul\\u00E1tk\\u00F3 for their help with the porosity measurements. |
| Subjects: | Q Science / természettudomány > QD Chemistry / kémia |
| SWORD Depositor: | MTMT SWORD |
| Depositing User: | MTMT SWORD |
| Date Deposited: | 23 Sep 2025 12:43 |
| Last Modified: | 23 Sep 2025 12:43 |
| URI: | https://real.mtak.hu/id/eprint/224966 |
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