Related Experiment Video
Updated: Jun 28, 2025
09:36
Polyethyleneimine-coated Iron Oxide Nanoparticles as a Vehicle for the Delivery of Small Interfering RNA to Macrophages In Vitro and In Vivo
Published on: February 5, 2019
8.7K
Spray-drying of PEI-/PPI-based nanoparticles for DNA or siRNA delivery.
Sandra Noske1, Michael Karimov1, Martin Krüger2
1Rudolf-Boehm-Institute for Pharmacology and Toxicology, Clinical Pharmacology, Leipzig University, Faculty of Medicine, Härtelstraße 16-18, 04107 Leipzig, Germany.
Summary
Spray-drying of nucleic acid nanoparticles, using poly(vinyl alcohol) as an excipient, yields stable, effective dry powders for gene therapy. These optimized formulations enhance storage and enable direct pulmonary drug delivery.
Area of Science:
- Biotechnology and Pharmaceutical Sciences
- Nanotechnology for Drug Delivery
- Gene Therapy Formulations
Background:
- Spray-drying offers advantages for nucleic acid drug formulation, including enhanced stability and potential for pulmonary delivery.
- Encapsulating nucleic acids in nanoparticles before spray-drying is crucial for effective formulations.
- Polyethylenimine (PEI)-based nanoparticles, especially tyrosine-modified versions, show promise for gene delivery due to stability and efficacy.
Purpose of the Study:
- To determine optimal spray-drying conditions for polyethylenimine (PEI)-based nanoparticles containing plasmid DNA or small interfering RNAs (siRNAs).
- To evaluate the suitability of different excipients, focusing on poly(vinyl alcohol) (PVA), for spray-drying nucleic acid nanoparticles.
- To investigate the impact of spray-drying on nanoparticle characteristics and their subsequent efficacy.
Main Methods:
- Optimization of spray-drying parameters including mesh size and temperature for PEI-DNA/siRNA nanoparticles.
- Evaluation of various excipients (PVA, trehalose, lactose) for their effect on nanoparticle formulation and function.
- Characterization of spray-dried microparticles and released nanoparticles using laser granulometry and zeta potential measurements.
- Assessment of transfection efficacy of fresh versus spray-dried nanoparticles.
Main Results:
- Poly(vinyl alcohol) (PVA) was identified as a superior excipient, maintaining or improving transfection efficacy compared to fresh complexes.
- Optimal spray-drying involved a large mesh size; temperature variation had a minor impact.
- Spray-dried microparticles ranged from approximately 3.3 to 8.5 µm, with nanoparticles exhibiting increased size and altered zeta potentials post-reconstitution.
- Spray-dried nanoparticles retained high efficacy even after prolonged storage.
Conclusions:
- Spray-dried PEI-based nanoparticle systems offer a promising approach for stable nucleic acid drug storage and facile reconstitution.
- These formulations are suitable for direct pulmonary application as dry powders, expanding therapeutic delivery options.
- The optimized spray-drying process, particularly with PVA, enhances the potential of nucleic acid-based therapeutics.
