Next Article in Journal
Gene Therapy for Regenerative Medicine
Next Article in Special Issue
Development of Nanofibers with Embedded Liposomes Containing an Immunomodulatory Drug Using Green Electrospinning
Previous Article in Journal
Multifunctional Mesoporous Silica-Coated Gold Nanorods Mediate Mild Photothermal Heating-Enhanced Gene/Immunotherapy for Colorectal Cancer
Previous Article in Special Issue
Electrospinning of Potential Medical Devices (Wound Dressings, Tissue Engineering Scaffolds, Face Masks) and Their Regulatory Approach
 
 
Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
Journals
Pharmaceutics
Volume 15
Issue 3
10.3390/pharmaceutics15030855
pharmaceutics-logo
Submit to this Journal Review for this Journal Propose a Special Issue
► Article Menu

Article Menu

share Share announcement Help format_quote Cite question_answer Discuss in SciProfiles
first_page
settings
Order Article Reprints
Font Type:
Arial Georgia Verdana
Font Size:
Aa Aa Aa
Line Spacing:
Column Width:
Background:
Article

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

by
Edit Hirsch
1,*,
Márió Nacsa
1,
Eszter Pantea
1,
Edina Szabó
1,
Panna Vass
1,
Júlia Domján
1,
Attila Farkas
1,
Zoltán Nyíri
2,
Zsuzsanna Eke
2,
Tamás Vigh
3,
Sune Klint Andersen
3,
Geert Verreck
3,
György János Marosi
1 and
Zsombor Kristóf Nagy
1
1
Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Müegyetem rkp. 3, 1111 Budapest, Hungary
2
Joint Research and Training Laboratory on Separation Techniques, Eötvös Loránd University, Pázmány Péter stny. 1/A, 1117 Budapest, Hungary
3
Oral Solids Development, Janssen R&D, Turnhoutseweg 30, B-2340 Beerse, Belgium
*
Author to whom correspondence should be addressed.
Pharmaceutics 2023, 15(3), 855; https://doi.org/10.3390/pharmaceutics15030855
Submission received: 27 January 2023 / Revised: 16 February 2023 / Accepted: 2 March 2023 / Published: 6 March 2023
(This article belongs to the Special Issue Recent Development of Electrospinning for Drug Delivery, 3rd Edition)
Browse Figures
Versions Notes

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.
Keywords: biopharmaceutical formulation; electrospinning; solvent optimization; downstream processing; high-drug-loaded fibers; antisense oligonucleotide; oral delivery biopharmaceutical formulation; electrospinning; solvent optimization; downstream processing; high-drug-loaded fibers; antisense oligonucleotide; oral delivery
Graphical Abstract

Share and Cite

MDPI and ACS Style

Hirsch, E.; Nacsa, M.; Pantea, E.; Szabó, E.; Vass, P.; Domján, J.; Farkas, A.; Nyíri, Z.; Eke, Z.; Vigh, T.; et al. Oligonucleotide Formulations Prepared by High-Speed Electrospinning: Maximizing Loading and Exploring Downstream Processability. Pharmaceutics 2023, 15, 855. https://doi.org/10.3390/pharmaceutics15030855

AMA Style

Hirsch E, Nacsa M, Pantea E, Szabó E, Vass P, Domján J, Farkas A, Nyíri Z, Eke Z, Vigh T, et al. Oligonucleotide Formulations Prepared by High-Speed Electrospinning: Maximizing Loading and Exploring Downstream Processability. Pharmaceutics. 2023; 15(3):855. https://doi.org/10.3390/pharmaceutics15030855

Chicago/Turabian Style

Hirsch, Edit, Márió Nacsa, Eszter Pantea, Edina Szabó, Panna Vass, Júlia Domján, Attila Farkas, Zoltán Nyíri, Zsuzsanna Eke, Tamás Vigh, and et al. 2023. "Oligonucleotide Formulations Prepared by High-Speed Electrospinning: Maximizing Loading and Exploring Downstream Processability" Pharmaceutics 15, no. 3: 855. https://doi.org/10.3390/pharmaceutics15030855

APA Style

Hirsch, E., Nacsa, M., Pantea, E., Szabó, E., Vass, P., Domján, J., Farkas, A., Nyíri, Z., Eke, Z., Vigh, T., Andersen, S. K., Verreck, G., Marosi, G. J., & Nagy, Z. K. (2023). Oligonucleotide Formulations Prepared by High-Speed Electrospinning: Maximizing Loading and Exploring Downstream Processability. Pharmaceutics, 15(3), 855. https://doi.org/10.3390/pharmaceutics15030855

Note that from the first issue of 2016, this journal uses article numbers instead of page numbers. See further details here.

Article Metrics

Back to TopTop