Spray drying from organic solvents to prepare nanoporous/nanoparticulate microparticles of protein: excipient composites designed for oral inhalation

Ní Ógáin, O; Tajber, L; Corrigan, OI; Healy, AM

HERO ID

1445007

Reference Type

Journal Article

Year

2012

Language

English

PMID

22881440

HERO ID 1445007
In Press No
Year 2012
Title Spray drying from organic solvents to prepare nanoporous/nanoparticulate microparticles of protein: excipient composites designed for oral inhalation
Authors Ní Ógáin, O; Tajber, L; Corrigan, OI; Healy, AM
Journal Journal of Pharmacy and Pharmacology
Volume 64
Issue 9
Page Numbers 1275-1290
Abstract <strong>OBJECTIVES: </strong>The aim of this study was to determine if spray-drying could successfully produce microparticles containing the model protein trypsin in a form suitable for inhalation.<br /><br /><strong>METHODS: </strong>Trypsin was spray-dried with raffinose from a methanol : n-butyl acetate solvent system (MeOH : BA). The solvent system was then adjusted to include water, and trypsin was co-spray-dried with raffinose, trehalose or hydroxpropyl-β-cyclodextrin. The spray-dried products were characterised by SEM, XRD, DSC, TGA and FTIR. Protein biological activity and in-vitro deposition of trypsin : excipient nanoporous/nanoparticulate microparticles (NPMPs) was also assessed.<br /><br /><strong>KEY FINDINGS: </strong>The inclusion of water in a MeOH : BA solvent system allowed for the successful production of NPMPs of trypsin : excipient by spray-drying. Trypsin formulated as trypsin : excipient NPMPs retained biological activity on processing and showed no deterioration in activity or morphological characteristics when stored with desiccant at either 4 or 25°C. Hydroxpropyl-β-cyclodextrin showed advantages over the sugars in terms of producing powders with appropriate density and with greater physical stability under high-humidity conditions. Fine particle fractions of between 41 and 45% were determined for trypsin : excipient NPMPs.<br /><br /><strong>CONCLUSIONS: </strong>NPMPs of trypsin : excipient systems can be produced by spray-drying by adjustment of the solvent system to allow for adequate solubility of trypsin.
Doi 10.1111/j.2042-7158.2012.01488.x
Pmid 22881440
Wosid WOS:000307217900008
Is Certified Translation No
Dupe Override No
Comments Source: Web of Science WOS:000307217900008
Is Public Yes
Language Text English
Keyword inhalation; nanoporous; nanoparticulate microparticles; spray-drying; trypsin