1. A comparison of acyl-moieties for noncovalent functionalization of PLGA and PEG-PLGA nanoparticles with a cell-penetrating peptide
- Author
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Marc Schneider, Karl-Heinz Wiesmüller, Rike Nabbefeld, Andreas Kirchner, Muhanad Ali, X. Frank Walboomers, Daniel Primavessy, Roland Brock, Omar Paulino da Silva Filho, Silko Grimm, and Petra H. M. Bovee-Geurts
- Subjects
chemistry.chemical_classification ,General Chemical Engineering ,technology, industry, and agriculture ,Nanoparticle ,Peptide ,General Chemistry ,Acylation ,PLGA ,chemistry.chemical_compound ,All institutes and research themes of the Radboud University Medical Center ,Reconstructive and regenerative medicine Radboud Institute for Molecular Life Sciences [Radboudumc 10] ,chemistry ,PEG ratio ,Biophysics ,Cell-penetrating peptide ,Nanomedicine ,Surface modification ,Nanomedicine Radboud Institute for Molecular Life Sciences [Radboudumc 19] - Abstract
Efficient intracellular drug delivery in nanomedicine strongly depends on ways to induce cellular uptake. Conjugation of nanoparticles (NPs) with cell-penetrating peptides (CPPs) is a known means to induce uptake via endocytosis. Here, we functionalized NPs consisting of either poly(D,L-lactide-co-glycolide) (PLGA) or polyethene glycol (PEG)-PLGA block-copolymer with a lactoferrin-derived cell-penetrating peptide (hLF). To enhance the association between the peptide and the polymer NPs, we tested a range of acyl moieties for N-terminal acylation of the peptide as a means to promote noncovalent interactions. Acyl moieties differed in chain length and number of acyl chains. Peptide-functionalized NPs were characterized for nanoparticle size, overall net charge, storage stability, and intracellular uptake. Coating particles with a palmitoylated hLF resulted in minimal precipitation after storage at −20C and homogeneous particle size (
- Published
- 2021