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Nanoscale characterization of PEGylated phospholipid coatings formed by spray drying on silica microparticles
Uppsala Univ, Dept Pharm, Uppsala, Sweden..
KTH, School of Engineering Sciences (SCI), Applied Physics, Nanostructure Physics.ORCID iD: 0000-0003-0675-974X
Orexo AB, Pharmaceut Dev, Uppsala, Sweden..
AstraZeneca, Early Prod Dev & Mfg Pharmaceut Sci, R&D, Gothenburg, Sweden..
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2020 (English)In: Journal of Colloid and Interface Science, ISSN 0021-9797, E-ISSN 1095-7103, Vol. 577, p. 92-100Article in journal (Refereed) Published
Abstract [en]

Phospholipids constitute biocompatible and safe excipients for pulmonary drug delivery. They can retard the drug release and, when PEGylated, also prolong the residence time in the lung. The aim of this work was to assess the structure and coherence of phospholipid coatings formed by spray drying on hydrophilic surfaces (silica microparticles) on the nanoscale and, in particular, the effect of addition of PEGylated lipids thereon. Scanning electron microscopy showed the presence of nanoparticles of varying sizes on the microparticles with different PEGylated lipid concentrations. Atomic force microscopy confirmed the presence of a lipid coating on the spray-dried microparticles. It also revealed that the lipid-coated microparticles without PEGylated lipids had a rather homogenous coating whereas those with PEGylated lipids had a very heterogeneous coating with defects, which was corroborated by confocal laser scanning microscopy. All coated microparticles had good dispersibility without agglomerate formation, as indicated by particle size measurements. This study has demonstrated that coherent coatings of phospholipids on hydrophilic surfaces can be obtained by spray drying. However, the incorporation of PEGylated lipids in a one-step spray-drying process to prepare lipid coated microparticles with both controlled-release and stealth properties is very challenging.

Place, publisher, year, edition, pages
Elsevier BV , 2020. Vol. 577, p. 92-100
Keywords [en]
Solid lipid microparticle, Lipid coated microparticle, Controlled release, PEGylated microparticle, PEGylated surface, Spray drying, Pulmonary dry powder
National Category
Physical Chemistry
Identifiers
URN: urn:nbn:se:kth:diva-279388DOI: 10.1016/j.jcis.2020.05.045ISI: 000556588700012PubMedID: 32473480Scopus ID: 2-s2.0-85085254178OAI: oai:DiVA.org:kth-279388DiVA, id: diva2:1462250
Note

QC 20200828

Available from: 2020-08-28 Created: 2020-08-28 Last updated: 2022-06-25Bibliographically approved

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Forchheimer, Daniel

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