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Article

Quantification of Surface GalNAc Ligands Decorating Nanostructured Lipid Carriers by UPLC-ELSD

by
Laura Gauthier
1,2,
Mathieu Varache
1,
Anne-Claude Couffin
1,
Colette Lebrun
2,
Pascale Delangle
2,
Christelle Gateau
2,* and
Isabelle Texier
1,*
1
Université Grenoble Alpes, CEA, LETI-DTBS, F-38000 Grenoble, France
2
Université Grenoble Alpes, CEA, CNRS, IRIG-SyMMES, F-38000 Grenoble, France
*
Authors to whom correspondence should be addressed.
Int. J. Mol. Sci. 2019, 20(22), 5669; https://doi.org/10.3390/ijms20225669
Submission received: 24 September 2019 / Revised: 7 November 2019 / Accepted: 9 November 2019 / Published: 12 November 2019
(This article belongs to the Special Issue Surface-Functionalized Nanoparticles as Drug Carriers)
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Abstract

Nanoparticles have been extensively studied for drug delivery and targeting to specific organs. The functionalization of the nanoparticle surface by site-specific ligands (antibodies, peptides, saccharides) can ensure efficient recognition and binding with relevant biological targets. One of the main challenges in the development of these decorated nanocarriers is the accurate quantification of the amount of ligands on the nanoparticle surface. In this study, nanostructured lipid carriers (NLC) were functionalized with N-acetyl-D-galactosamine (GalNAc) units, known to target the asialoglycoprotein receptor (ASGPR). Different molar percentages of GalNAc-functionalized surfactant (0%, 2%, 5%, and 14%) were used in the formulation. Based on ultra-high-performance liquid chromatography separation and evaporative light-scattering detection (UPLC-ELSD), an analytical method was developed to specifically quantify the amount of GalNAc units present at the NLC surface. This method allowed the accurate quantification of GalNAc surfactant and therefore gave some insights into the structural parameters of these multivalent ligand systems. Our data show that the GalNAc decorated NLC possess large numbers of ligands at their surface and suitable distances between them for efficient multivalent interaction with the ASGPR, and therefore promising liver-targeting efficiency.
Keywords: nanostructured lipid carriers; N-acetyl-D-galactosamine ligand; surface functionalization; ligand quantification nanostructured lipid carriers; N-acetyl-D-galactosamine ligand; surface functionalization; ligand quantification

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MDPI and ACS Style

Gauthier, L.; Varache, M.; Couffin, A.-C.; Lebrun, C.; Delangle, P.; Gateau, C.; Texier, I. Quantification of Surface GalNAc Ligands Decorating Nanostructured Lipid Carriers by UPLC-ELSD. Int. J. Mol. Sci. 2019, 20, 5669. https://doi.org/10.3390/ijms20225669

AMA Style

Gauthier L, Varache M, Couffin A-C, Lebrun C, Delangle P, Gateau C, Texier I. Quantification of Surface GalNAc Ligands Decorating Nanostructured Lipid Carriers by UPLC-ELSD. International Journal of Molecular Sciences. 2019; 20(22):5669. https://doi.org/10.3390/ijms20225669

Chicago/Turabian Style

Gauthier, Laura, Mathieu Varache, Anne-Claude Couffin, Colette Lebrun, Pascale Delangle, Christelle Gateau, and Isabelle Texier. 2019. "Quantification of Surface GalNAc Ligands Decorating Nanostructured Lipid Carriers by UPLC-ELSD" International Journal of Molecular Sciences 20, no. 22: 5669. https://doi.org/10.3390/ijms20225669

APA Style

Gauthier, L., Varache, M., Couffin, A.-C., Lebrun, C., Delangle, P., Gateau, C., & Texier, I. (2019). Quantification of Surface GalNAc Ligands Decorating Nanostructured Lipid Carriers by UPLC-ELSD. International Journal of Molecular Sciences, 20(22), 5669. https://doi.org/10.3390/ijms20225669

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