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Porous Silicon Microparticles for Delivery of siRNA Therapeutics
Published on: January 15, 2015
SPANosomes as delivery vehicles for small interfering RNA (siRNA)
Chenguang Zhou1, Yicheng Mao, Yasuro Sugimoto
1Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, USA.
Molecular Pharmaceutics
|December 14, 2011
Summary
Novel nonionic surfactant vesicles, or SPANosomes (SPs), effectively deliver small interfering RNA (siRNA) into breast cancer cells. These SPANosomes demonstrate efficient gene silencing and endosomal escape, highlighting their potential as siRNA delivery vectors.
Area of Science:
- Biotechnology
- Nanotechnology
- Molecular Biology
Background:
- Nonionic surfactant vesicles (SPANosomes) are investigated for drug delivery applications.
- Cationic lipids and sorbitan monooleate (Span 80) are key components in SPANosome formulation.
- Small interfering RNA (siRNA) holds therapeutic potential but requires effective delivery systems.
Purpose of the Study:
- To synthesize and evaluate SPANosomes as vectors for siRNA delivery.
- To assess the physicochemical properties and colloidal stability of SPANosomes.
- To determine the gene silencing efficiency and cellular uptake mechanism of SP/siRNA complexes.
Main Methods:
- SPANosomes were synthesized using cationic lipid and Span 80.
- Physicochemical characterization included size, zeta potential, and colloidal stability assessment.
- Cryogenic transmission electron microscopy (cryo-TEM) visualized SP/siRNA complex structure.
- Gene silencing efficacy was evaluated using green fluorescent protein (GFP) and aromatase assays.
- Confocal microscopy with molecular beacons tracked cellular trafficking and endosomal escape.
Main Results:
- Synthesized SPANosomes had a mean diameter <100 nm and excellent colloidal stability.
- SP/siRNA complexes showed a positive zeta potential (+12 mV) and high siRNA incorporation (>80%).
- Cryo-TEM revealed a core-shell structure for SP/siRNA complexes.
- Efficient and specific gene silencing was achieved: 66% for GFP and 77% for aromatase.
- Confocal microscopy confirmed efficient endosomal escape and cytosolic delivery of siRNA.
Conclusions:
- Span 80 acts as a potent helper lipid in SPANosome formulation.
- SPANosomes are promising, stable, and efficient nanocarriers for siRNA delivery.
- The SPANosome system facilitates endosomal escape and cytosolic delivery of siRNA cargo.
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