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Polycaprolactone microspheres as carriers for dry powder inhalers : effect of surface coating on aerosolization of salbutamol sulfate

Tuli, Rinku A., Dargaville, Tim R., George, Graeme A., & Islam, Nazrul (2012) Polycaprolactone microspheres as carriers for dry powder inhalers : effect of surface coating on aerosolization of salbutamol sulfate. Journal of Pharmaceutical Sciences, 101(2), pp. 733-745.

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    Abstract

    This study reports the factors controlling aerosolization of salbutamol sulfate (SS) from mixtures with polycaprolactone (PCL) microspheres fabricated using an emulsion technique with polyvinyl alcohol (PVA) as stabilizer. The fine particle fraction (FPF) of SS from PCL measured by a twin-stage impinger was unexpectedly found to be zero, although scanning electron microscopy showed that the drug coated the entire microsphere. Precoating the microspheres with magnesium stearate (MgSt) excipient solutions (1%–2%) significantly increased (p < 0.05, n = 5) the FPF of SS (11.4%–15.4%), whereas precoating with leucine had a similar effect (FPF = 11.3 ± 1.1%), but was independent of the solution concentration. The force of adhesion (by atomic force microscopy) between the PCL microspheres and SS was reduced from 301.4 ± 21.7 nN to 110.9 ± 30.5 nN and 121.8 ± 24.6 nN, (p < 0.05, n = 5) for 1% and 2% MgSt solutions, respectively, and to 148.1 ± 21.0 nN when coated with leucine. The presence of PVA on the PCL microspheres (detected by X-ray photoelectron spectroscopy) affected the detachment of SS due to strong adhesion between the two, presumably due to capillary forces acting between them. Precoating the microspheres with excipients increased the FPF significantly by reducing the drug–carrier adhesion. © 2011 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:733–745, 2012

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    2 citations in Web of Science®

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    ID Code: 47719
    Item Type: Journal Article
    Keywords: Biodegradable polymers, Pulmonary drug delivery, Microparticles, Aerosols, Polymeric drug carrier
    DOI: 10.1002/jps.22777
    ISSN: 0022-3549
    Subjects: Australian and New Zealand Standard Research Classification > MEDICAL AND HEALTH SCIENCES (110000) > PHARMACOLOGY AND PHARMACEUTICAL SCIENCES (111500)
    Divisions: Past > Schools > Chemistry
    Past > QUT Faculties & Divisions > Faculty of Science and Technology
    Current > Institutes > Institute of Health and Biomedical Innovation
    Past > Schools > Pharmacy
    Copyright Owner: Copyright 2011 Wiley Periodicals, Inc. and the American Pharmacists Association
    Deposited On: 14 Dec 2011 13:20
    Last Modified: 21 Mar 2013 20:37

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