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Updated: Feb 10, 2026

Targeting Drugs to Larval Zebrafish Macrophages by Injecting Drug-Loaded Liposomes
Published on: February 18, 2020
Pentaglycine lipid derivates - rp-HPLC analytics for bioorthogonal anchor molecules in targeted, multiple-composite
Steffen Wöll1, Stefan Schiller2, Christopher Bachran3
1Merck KGaA, Frankfurter Str. 250, 64293 Darmstadt, Germany; Department of Pharmaceutics and Biopharmaceutics, Kiel University, Grasweg 9a, 24118 Kiel, Germany.
Abstract:
The quantification of lipids and assessment of lipid composition is an indispensable step during the pharmaceutical development of novel lipid based drug delivery systems such as liposomes. Broad excipient screenings of such formulations raise the need for versatile analytical methods. Even more demanding complexity is generated by introduction of targeted systems requiring functionalized lipids. We addressed this demand by developing an rp-HPLC based analytical method with evaporative light scattering detection (ELSD) for the simultaneous analysis of commonly used phosphatidylcholines, cholesterol and bilayer surface-modifying cationic, anionic or PEGylated lipids, which can be analyzed in combination with novel pentaglycine lipids suitable as targeting ligand anchor. The method was validated for specificity, precision, accuracy and sample stability. We monitor the continuous and scalable manufacturing of two pentaglycine-modified liposomal formulations and track the modification of these drug delivery systems with a single-domain antibody utilizing bioorthogonal Sortase-A technology. Both the presented analytical and preparative techniques can help to improve the quality control and to accelerate the pharmaceutical development of such targeted drug delivery systems.
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