Evidence map›Paper›PMID 36986716›Full record

ArticlePharmaceutics2023

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

Edit Hirsch, Márió Nacsa, Eszter Pantea, Edina Szabó, Panna Vass, Júlia Domján, Attila Farkas, Zoltán Nyíri, Zsuzsanna Eke, Tamás Vigh and 4 more

Open access · goldAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Pharmaceutics, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
0.5field-weighted citation impact, top 42% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

0 citing papers in PubMed, 5 citations in OpenAlex.

No citing paper in PubMed yet.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

14 authors at 3 institutions in 2 countries.

Edit HirschDepartment of Organic Chemistry and Technology, Budapest University of Technology and Economics, Müegyetem rkp. 3, 1111 Budapest, Hungary.ORCID 0000-0002-4672-9572
Márió NacsaDepartment of Organic Chemistry and Technology, Budapest University of Technology and Economics, Müegyetem rkp. 3, 1111 Budapest, Hungary.
Eszter PanteaDepartment of Organic Chemistry and Technology, Budapest University of Technology and Economics, Müegyetem rkp. 3, 1111 Budapest, Hungary.
Edina SzabóDepartment of Organic Chemistry and Technology, Budapest University of Technology and Economics, Müegyetem rkp. 3, 1111 Budapest, Hungary.
Panna VassDepartment of Organic Chemistry and Technology, Budapest University of Technology and Economics, Müegyetem rkp. 3, 1111 Budapest, Hungary.
Júlia DomjánDepartment of Organic Chemistry and Technology, Budapest University of Technology and Economics, Müegyetem rkp. 3, 1111 Budapest, Hungary.ORCID 0000-0001-5040-751X
Attila FarkasDepartment of Organic Chemistry and Technology, Budapest University of Technology and Economics, Müegyetem rkp. 3, 1111 Budapest, Hungary.ORCID 0000-0002-8877-2587
Zoltán NyíriJoint Research and Training Laboratory on Separation Techniques, Eötvös Loránd University, Pázmány Péter stny. 1/A, 1117 Budapest, Hungary.ORCID 0000-0003-4276-4036
Zsuzsanna EkeJoint Research and Training Laboratory on Separation Techniques, Eötvös Loránd University, Pázmány Péter stny. 1/A, 1117 Budapest, Hungary.
Tamás VighOral Solids Development, Janssen R&D, Turnhoutseweg 30, B-2340 Beerse, Belgium.
Sune Klint AndersenOral Solids Development, Janssen R&D, Turnhoutseweg 30, B-2340 Beerse, Belgium.
Geert VerreckOral Solids Development, Janssen R&D, Turnhoutseweg 30, B-2340 Beerse, Belgium.
György János MarosiDepartment of Organic Chemistry and Technology, Budapest University of Technology and Economics, Müegyetem rkp. 3, 1111 Budapest, Hungary.
Zsombor Kristóf NagyDepartment of Organic Chemistry and Technology, Budapest University of Technology and Economics, Müegyetem rkp. 3, 1111 Budapest, Hungary.ORCID 0000-0003-2651-7756
Budapest University of Technology and Economics · HUJanssen (Belgium) · BEEötvös Loránd University · HU

Funding

Ministry for Innovation and Technology TKP2021-EGA-02Ministry for Innovation and Technology ÚNKP-21-4-II-BME-331
6 · The paper itself

Abstract

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.

Indexed as

antisense oligonucleotidebiopharmaceutical formulationdownstream processingelectrospinninghigh-drug-loaded fibersoral deliverysolvent optimization

Identifiers

PMID36986716
PMCPMC10054037
OpenAlexW4323313306

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.