Magnetised Thermo Responsive Lipid Vehicles for Targeted and Controlled Lung Drug Delivery
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- Upadhyay, D., Scalia, S., Vogel, R. et al. Pharm Res (2012) 29: 2456. doi:10.1007/s11095-012-0774-9
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Conditions such as lung cancer currently lack non-invasively targetable and controlled release topical inhalational therapies. Superparamagnetic iron-oxide nanoparticles (SPIONs) have shown promising results as a targetable therapy. We aimed to fabricate and test the in-vitro performance of particles with SPION and drug within a lipid matrix as a potentially targetable and thermo-sensitive inhalable drug-delivery system.
Budesonide and SPIONs were incorporated into lipid particles using oil-in-water emulsification. Particles size, chemical composition, responsiveness to magnetic field, thermosensitiveness and inhalation performance in-vitro were investigated.
Particles of average diameter 2–4 μm with budesonide and SPIONs inside the lipid matrix responded to a magnetic field with 100% extraction at a distance of 5 mm. Formulations were shown to have accelerated rate of drug release at hyperthermic temperatures (45°C)—controlled release. The produced inhalation dry powder presented promising inhalation performance, with an inhalable fine particle fraction of 30%.
The lipid system presented thermo-sensitive characteristics, suitable for controlled delivery, the model drug and SPION loaded lipid system was magnetically active and movable using simple permanent magnets, and the system demonstrates promise as an effective drug vehicle in targeted and controlled inhalation therapy.
KEY WORDScontrolled drug deliveryinhalationiron oxidelipidmagneto-responsivethermo-responsivetriggered drug release
acrylonitrile butadiene styrene thermoplastic
atomic forced microscopy
dry powder for inhalation
differential scanning calorimetry
energy-dispersing X-ray analysis
budesonide containing lipid microcapsules
budesonide and SPION containing lipid microcapsules
glyceryl behenate (Compritol 888)
scanning electron microscopy
scanning ion occlusion sensing
superparamagnetic iron-oxide nanoparticles