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Magnetised Thermo Responsive Lipid Vehicles for Targeted and Controlled Lung Drug Delivery

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ABSTRACT

Purpose

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.

Methods

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.

Results

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%.

Conclusions

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.

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Abbreviations

ABST:

acrylonitrile butadiene styrene thermoplastic

AFM:

atomic forced microscopy

DPI:

dry powder for inhalation

DSC:

differential scanning calorimetry

EDX:

energy-dispersing X-ray analysis

HPMC:

hydroxypropyl methylcellulose

Lip-Bud:

budesonide containing lipid microcapsules

Lip-Bud-SPION:

budesonide and SPION containing lipid microcapsules

Lipid:

glyceryl behenate (Compritol 888)

logP:

partition coefficient

SEM:

scanning electron microscopy

SIOS:

scanning ion occlusion sensing

SPION:

superparamagnetic iron-oxide nanoparticles

XRD:

X-ray diffraction

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Author information

Authors and Affiliations

  1. The University of Sydney, The Faculty of Pharmacy, Pharmacy Building A15, Sydney, NSW, 2006, Australia

    Dhrumil Upadhyay, Rania O. Salama, Paul M. Young, Daniela Traini & Wojciech Chrzanowski

  2. Department of Pharmaceutical Sciences, Ferrara University, 44121, Ferrara, Italy

    Santo Scalia

  3. Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, 161 Cathedral Street, G4 0RE, Glasgow, United Kingdom

    Nial Wheate

  4. School of Mathematics and Physics, The University of Queensland, St Lucia, Qld, 4072, Australia

    Robert Vogel

  5. Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt

    Rania O. Salama

Authors
  1. Dhrumil Upadhyay
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  2. Santo Scalia
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  3. Robert Vogel
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  4. Nial Wheate
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  6. Paul M. Young
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  8. Wojciech Chrzanowski
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Correspondence to Wojciech Chrzanowski.

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Upadhyay, D., Scalia, S., Vogel, R. et al. Magnetised Thermo Responsive Lipid Vehicles for Targeted and Controlled Lung Drug Delivery. Pharm Res 29, 2456–2467 (2012). https://doi.org/10.1007/s11095-012-0774-9

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  • DOI: https://doi.org/10.1007/s11095-012-0774-9

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