Continuous downstream processing of milled electrospun fibers to tablets monitored by near-infrared and Raman spectroscopy

Szabó, Edina; Záhonyi, Petra; Gyürkés, Martin; Nagy, Brigitta; Galata, Dorián László; Madarász, Lajos; Hirsch, Edit; Farkas, Attila; Andersen, Sune Klint; Vígh, Tamás; Verreck, Geert; Csontos, István; Marosi, György; Nagy, Zsombor Kristóf

doi:10.1016/j.ejps.2021.105907

Cited by 10 publications

(2 citation statements)

References 57 publications

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“…Fülöp et al [ 23 ] showed that it is possible to prepare low-dose tablets with acceptable content uniformity from electrospun drug-loaded fibre mats after high-shear dry mixing with conventional tabletting excipients on a reasonable development lab scale (500 g) and compression on a rotary tablet press. Szabó et al [ 24 ] successfully applied continuous manufacturing processing techniques (mixing, compression) with inline analysis to prepare tablets from electrospun drug-loaded microfibre mats; in this case, the milled fibres were treated as a starting material. A detailed study on the mechanical and compression behaviour of electrospun drug-loaded nanofibre mats has recently been published [ 25 ].…”

Section: Introductionmentioning

confidence: 99%

Development of Robust Tablet Formulations with Enhanced Drug Dissolution Profiles from Centrifugally-Spun Micro-Fibrous Solid Dispersions of Itraconazole, a BCS Class II Drug

et al. 2023

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Fibre-based oral drug delivery systems are an attractive approach to addressing low drug solubility, although clear strategies for incorporating such systems into viable dosage forms have not yet been demonstrated. The present study extends our previous work on drug-loaded sucrose microfibres produced by centrifugal melt spinning to examine systems with high drug loading and investigates their incorporation into realistic tablet formulations. Itraconazole, a model BCS Class II hydrophobic drug, was incorporated into sucrose microfibres at 10, 20, 30, and 50% w/w. Microfibres were exposed to high relative humidity conditions (25 °C/75% RH) for 30 days to deliberately induce sucrose recrystallisation and collapse of the fibrous structure into powdery particles. The collapsed particles were successfully processed into pharmaceutically acceptable tablets using a dry mixing and direct compression approach. The dissolution advantage of the fresh microfibres was maintained and even enhanced after humidity treatment for drug loadings up to 30% w/w and, importantly, retained after compression into tablets. Variations in excipient content and compression force allowed manipulation of the disintegration rate and drug content of the tablets. This then permitted control of the rate of supersaturation generation, allowing the optimisation of the formulation in terms of its dissolution profile. In conclusion, the microfibre-tablet approach has been shown to be a viable method for formulating poorly soluble BCS Class II drugs with improved dissolution performance.

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Section: Introductionmentioning

confidence: 99%

Development of Robust Tablet Formulations with Enhanced Drug Dissolution Profiles from Centrifugally-Spun Micro-Fibrous Solid Dispersions of Itraconazole, a BCS Class II Drug

et al. 2023

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“…In addition, HSES connected to a cyclone was demonstrated to be a feasible solution for the continuous collection of fibers [ 34 ]. The conversion of electrospun fibers into oral tablets, as a final dosage form, requires adequate downstream processability (e.g., grindability), but the manufacture of tablets is especially challenging due to the physical properties of the fibers, such as low bulk density and poor flowability [ 35 ].…”

Section: Introductionmentioning

confidence: 99%

Oligonucleotide Formulations Prepared by High-Speed Electrospinning: Maximizing Loading and Exploring Downstream Processability

et al. 2023

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The aim of this study was to develop antisense oligonucleotide tablet formulations using high-speed electrospinning. Hydroxypropyl-beta-cyclodextrin (HPβCD) was used as a stabilizer and as an electrospinning matrix. In order to optimize the morphology of the fibers, electrospinning of various formulations was carried out using water, methanol/water (1:1), and methanol as solvents. The results showed that using methanol could be advantageous due to the lower viscosity threshold for fiber formation enabling higher potential drug loadings by using less excipient. To increase the productivity of electrospinning, high-speed electrospinning technology was utilized and HPβCD fibers containing 9.1% antisense oligonucleotide were prepared at a rate of ~330 g/h. Furthermore, to increase the drug content of the fibers, a formulation with a 50% drug loading was developed. The fibers had excellent grindability but poor flowability. The ground fibrous powder was mixed with excipients to improve its flowability, which enabled the automatic tableting of the mixture by direct compression. The fibrous HPβCD–antisense oligonucleotide formulations showed no sign of physical or chemical degradation over the 1-year stability study, which also shows the suitability of the HPβCD matrix for the formulation of biopharmaceuticals. The obtained results demonstrate possible solutions for the challenges of electrospinning such as scale-up and downstream processing of the fibers.

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Continuous twin-screw melt granulation of drug-loaded electrospun fibers

Záhonyi,

Müncz,

Péter-Haraszti

et al. 2025

European Journal of Pharmaceutics and Biopharmaceutics

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Continuous downstream processing of milled electrospun fibers to tablets monitored by near-infrared and Raman spectroscopy

Cited by 10 publications

References 57 publications

Development of Robust Tablet Formulations with Enhanced Drug Dissolution Profiles from Centrifugally-Spun Micro-Fibrous Solid Dispersions of Itraconazole, a BCS Class II Drug

Development of Robust Tablet Formulations with Enhanced Drug Dissolution Profiles from Centrifugally-Spun Micro-Fibrous Solid Dispersions of Itraconazole, a BCS Class II Drug

Oligonucleotide Formulations Prepared by High-Speed Electrospinning: Maximizing Loading and Exploring Downstream Processability

Continuous twin-screw melt granulation of drug-loaded electrospun fibers

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