Pharmaceutical Research

, Volume 29, Issue 9, pp 2456–2467

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

  • Dhrumil Upadhyay
  • Santo Scalia
  • Robert Vogel
  • Nial Wheate
  • Rania O. Salama
  • Paul M. Young
  • Daniela Traini
  • Wojciech Chrzanowski
Research Paper

DOI: 10.1007/s11095-012-0774-9

Cite this article as:
Upadhyay, D., Scalia, S., Vogel, R. et al. Pharm Res (2012) 29: 2456. doi:10.1007/s11095-012-0774-9

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.

KEY WORDS

controlled drug deliveryinhalationiron oxidelipidmagneto-responsivethermo-responsivetriggered drug release

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

Supplementary material

11095_2012_774_MOESM1_ESM.doc (778 kb)
ESM 1(DOC 778 kb)

Copyright information

© Springer Science+Business Media, LLC 2012

Authors and Affiliations

  • Dhrumil Upadhyay
    • 1
  • Santo Scalia
    • 2
  • Robert Vogel
    • 4
  • Nial Wheate
    • 3
  • Rania O. Salama
    • 1
    • 5
  • Paul M. Young
    • 1
  • Daniela Traini
    • 1
  • Wojciech Chrzanowski
    • 1
  1. 1.The University of Sydney, The Faculty of PharmacySydneyAustralia
  2. 2.Department of Pharmaceutical SciencesFerrara UniversityFerraraItaly
  3. 3.Strathclyde Institute of Pharmacy and Biomedical SciencesUniversity of StrathclydeGlasgowUnited Kingdom
  4. 4.School of Mathematics and PhysicsThe University of QueenslandSt LuciaAustralia
  5. 5.Faculty of PharmacyUniversity of AlexandriaAlexandriaEgypt