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The role of formulation approaches in presenting targeting ligands on lipid nanoparticles.

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Aims: The density of functional ligands on lipid nanoparticles (LNPs) greatly determined its capability of postfunctionalization and targetability for the applications of personalized nanomedicine and drug/gene delivery. This work is… Click to show full abstract

Aims: The density of functional ligands on lipid nanoparticles (LNPs) greatly determined its capability of postfunctionalization and targetability for the applications of personalized nanomedicine and drug/gene delivery. This work is to investigate whether and how formulation methods influence the presentation of surface ligands. Methods: Biotin-modified LNPs as a functional LNP model were synthesized by four different formulation methods. The biotin ligand density and targetability of biotin-LNPs were evaluated and compared. Results: Both the ligand density and targetability of biotin-LNPs formulated by four different formulation methods exhibited a similar trend: homogenization > extrusion > wave-shaped micromixer ≈ Y-shaped micromixer. Conclusion: Formulation methods could modulate the presentation of targeting ligands on LNPs, which could guide future formulation screening and nanomedicine engineering.

Keywords: targeting ligands; formulation; formulation methods; ligands lipid; biotin; lipid nanoparticles

Journal Title: Nanomedicine
Year Published: 2023

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