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Tetyczka, C; Hodzic, A; Kriechbaum, M; Juraić, K; Spirk, C; Hartl, S; Pritz, E; Leitinger, G; Roblegg, E.
Comprehensive characterization of nanostructured lipid carriers using laboratory and synchrotron X-ray scattering and diffraction.
Eur J Pharm Biopharm. 2019; 139(6):153-160
Doi: 10.1016/j.ejpb.2019.03.017
Web of Science
PubMed
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- Co-authors Med Uni Graz
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Leitinger Gerd
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Pritz Elisabeth
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The development of lipid nanoparticles requires knowledge on the crystalline structure, polymorphic transitions and lipid-drug interactions. This study aimed at introducing advanced techniques to characterize nanostructured lipid carriers (NLC) comprising palmitic acid, oleic acid, stabilizer and Domperidone. Crystallinity of single components and mixtures was investigated by laboratory Small Angle X-ray Scattering (SAXS). NLC were studied with laboratory Small and Wide Angle X-ray Scattering (SWAXS). Photon Correlation Spectroscopy and Freeze Fracture Transmission Electron Microscopy were used to monitor particle size, zeta potential and shape. Stability of NLC was investigated using synchrotron X-ray Diffraction (XRD) and SAXS and laboratory SAXS. Palmitic acid showed a lamellar structure (polymorph C), which was still present after particle preparation. Spherical 300 nm-sized particles with zeta potential values above -30 mV were obtained and Domperidone was incorporated in its amorphous form. During storage, no differences in synchrotron XRD spectra were seen. However, laboratory SAXS measurements showed a second lamellar structure, identified as polymorph B. Synchrotron SAXS temperature scans confirmed that polymorph B did not affect the morphology of the encapsulated drug or the shape of NLC. These results highlight the unique capabilities of laboratory and synchrotron X-ray Scattering and Diffraction for improved structural characterization of lipid nanoparticles.
Copyright © 2019 Elsevier B.V. All rights reserved.
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Nanostructured lipid carriers (NLC)
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Palmitic acid
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Laboratory small and wide angle X-ray scattering
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Synchrotron X-ray diffraction
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Synchrotron small angle X-ray scattering