Development of a spray congealing process for the preparation of insulin-loaded lipid microparticles and characterization thereof

Maschke, Angelika and Becker, Christian and Eyrich, Daniela and Kiermaier, Josef and Blunk, Torsten and Goepferich, Achim (2007) Development of a spray congealing process for the preparation of insulin-loaded lipid microparticles and characterization thereof. EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 65 (2). pp. 175-187. ISSN 0939-6411, 1873-3441

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Abstract

A spray congealing process for the preparation of protein-loaded microparticles was developed. The influence of the process parameters atomization pressure and spraying temperature on particle size and process yield was investigated by experimental design. The employed spray congealing technique enabled the production of microparticles with yields ranging from 79% to 95% and median particle sizes (d(0.5)) from 182.2 to 315 mu m. Insulin lipid microparticles could be prepared without any loss of insulin during the preparation process and the protein stability was not affected by the spray congealing process as investigated by HPLC-MS analysis. The stability of insulin encapsulated in lipid microparticles under release conditions over 28 days was assessed by investigating the residual insulin content. Starting after 3 days of release, a continuous increase of desamidoinsulin in the remaining particles of up to 7.5% after 28 days was observed. An additional degradation product was detected by HPLC and HPLC-MS analysis and identified as a covalent insulin dimer by MALDI-ToF. The microparticles did not show a burst release and testing the insulin lipid microparticles in a fibrin gel chondrocyte culture revealed that the released insulin was bioactive and had a significant effect on chondrocyte extracellular matrix production. (c) 2006 Elsevier B.V. All rights reserved.

Item Type: Article
Uncontrolled Keywords: SCANNING ELECTRON-MICROSCOPY; IN-VITRO RELEASE; TRANSFORMATION PRODUCTS; CHEMICAL-STABILITY; NANOPARTICLES; MICROSPHERES; MICROPELLETS; BEHAVIOR; STORAGE; MATRIX; spray congealing; lipid microparticles; controlled release; protein; insulin; experimental design
Subjects: 500 Science > 540 Chemistry & allied sciences
600 Technology > 615 Pharmacy
Divisions: Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Technology (Prof. Göpferich)
Chemistry and Pharmacy > Central Analytical Services
Depositing User: Dr. Gernot Deinzer
Date Deposited: 22 Dec 2020 11:03
Last Modified: 22 Dec 2020 11:03
URI: https://pred.uni-regensburg.de/id/eprint/33212

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