Molecularly designed lipid microdomains for solid dispersions using a polymer/inorganic carrier matrix produced by hot-melt extrusion
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Authors
Author (Corporation)
Publication date
29.02.2016
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Type
01A - Journal article
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Parent work
International Journal of Pharmaceutics
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DOI of the original publication
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Series
Series number
Volume
499
Issue / Number
1-2
Pages / Duration
90-100
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Publisher / Publishing institution
Elsevier
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Abstract
Amorphous solid dispersions have for many years been a focus in oral formulations, especially in combination with a hot-melt extrusion process. The present work targets a novel approach with a system based on a fatty acid, a polymer and an inorganic carrier. It was intended to adsorb the acidic lipid by specific molecular interactions onto the solid carrier to design disorder in the alkyl chains of the lipid. Such designed lipid microdomains (DLM) were created as a new microstructure to accommodate a compound in a solid dispersion. Vibrational spectroscopy, X-ray powder diffraction, atomic force microscopy as well as electron microscopic imaging were employed to study a system of stearic acid, hydroxypropylcellulose and aluminum magnesium silicate. β-carotene was used as a poorly water-soluble model substance that is difficult to formulate with conventional solid dispersion formulations. The results indicated that the targeted molecular excipient interactions indeed led to DLMs for specific compositions. The different methods provided complementary aspects and important insights into the created microstructure. The novel delivery system appeared to be especially promising for the formulation of oral compounds that exhibit both high crystal energy and lipophilicity.
Keywords
Acidic lipid, Designed lipid microdomains, Inorganic carrier, Interactions, Hot-melt extrusion
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ISBN
ISSN
0378-5173
1873-3476
1873-3476
Language
English
Created during FHNW affiliation
Yes
Strategic action fields FHNW
Publication status
Published
Review
Peer review of the complete publication
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License
Citation
Adler, C., Schönenberger, M., Teleki, A., & Kuentz, M. (2016). Molecularly designed lipid microdomains for solid dispersions using a polymer/inorganic carrier matrix produced by hot-melt extrusion. International Journal of Pharmaceutics, 499(1-2), 90–100. https://doi.org/10.1016/j.ijpharm.2015.12.057