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Oligonucleotide Formulations Prepared by High-Speed Electrospinning: Maximizing Loading and Exploring Downstream
Edit Hirsch1, Márió Nacsa1, Eszter Pantea1
1Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Müegyetem rkp. 3, 1111 Budapest, Hungary.
Pharmaceutics
|March 29, 2023
Summary
High-speed electrospinning successfully created antisense oligonucleotide (ASO) tablet formulations using hydroxypropyl-beta-cyclodextrin (HPβCD). This method offers a scalable solution for ASO drug delivery, demonstrating stability and potential for high drug loading.
Area of Science:
- Pharmaceutical Technology
- Biomaterials Engineering
- Drug Delivery Systems
Background:
- Antisense oligonucleotides (ASOs) are a promising class of therapeutics requiring effective delivery systems.
- Electrospinning offers potential for creating novel drug delivery matrices but faces challenges in scale-up and processing.
- Hydroxypropyl-beta-cyclodextrin (HPβCD) is explored as a stabilizer and matrix for electrospun formulations.
Purpose of the Study:
- To develop antisense oligonucleotide (ASO) tablet formulations utilizing high-speed electrospinning.
- To optimize electrospinning parameters for fiber morphology and productivity.
- To assess the stability and processability of the developed ASO-loaded HPβCD fibers for direct compression tableting.
Main Methods:
- Electrospinning of HPβCD with ASO using various solvents (water, methanol/water, methanol) to optimize fiber morphology.
- Utilization of high-speed electrospinning technology to achieve high production rates (~330 g/h).
- Formulation development for high drug loading (up to 50%) and subsequent processing including grinding, excipient addition, and direct compression tableting.
Main Results:
- Methanol as a solvent facilitated fiber formation with lower viscosity, enabling higher potential drug loading.
- High-speed electrospinning successfully produced HPβCD fibers containing 9.1% ASO at a high rate.
- Formulations with 50% drug loading were achieved; fibers exhibited good grindability but poor flowability, which was improved by excipient addition for successful tableting.
- The ASO-HPβCD formulations demonstrated excellent physical and chemical stability over a 1-year study period.
Conclusions:
- High-speed electrospinning is a viable and scalable technology for producing ASO-loaded HPβCD fibers for oral tablet formulations.
- HPβCD serves as a suitable matrix for stabilizing ASO and enabling high drug loading.
- The study provides solutions for electrospinning scale-up and downstream processing challenges, paving the way for biopharmaceutical manufacturing.
