Cell internalization kinetics and surface charge accessibility of surface-modified PAMAM dendrimers

Díaz, Carola F.; Cifuentes, Diego L.; Oyarzún, Maximiliano; Jiménez, Verónica A.; Guzmán, Leonardo

doi:10.1039/d3ob01265d

Org. Biomol. Chem.

2023

DOI: 10.1039/d3ob01265d

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Cell internalization kinetics and surface charge accessibility of surface-modified PAMAM dendrimers

Carola F. Díaz,

Diego L. Cifuentes,

Maximiliano Oyarzún

et al.

Abstract: The accessibility of surface cationic charges is a key determinant for the cell internalization capacity of surface-modified PAMAM dendrimers with acetyl, folate or poly(ethylene glycol) groups.

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2024

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Enhancement of octreotide antiproliferative activity by PEGylated PAMAM dendrimers delivery

Díaz,

Cifuentes,

Oyarzún

et al. 2024

J of Applied Polymer Sci

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PEGylated PAMAM dendrimers (PEG‐PAMAM) are well‐characterized biomaterials with still unexplored applications as carriers of drugs acting via membrane receptors, such as octreotide. This work confirmed the safety and negligible internalization capacity of fourth‐generation 50%‐PEG‐PAMAM in HEK‐293 cells, to then assessed their supramolecular binding to octreotide through tryptophan quenching experiments and Gaussian‐accelerated molecular dynamics (GaMD) simulations. Tryptophan quenching showed that PEG‐PAMAM binds octreotide with a Kbind of 6 × 106 M−1 and a complex stoichiometry of 1:1.4, unlike native PAMAM. GaMD simulations revealed that octreotide binds at the outer PEG shell of PEG‐PAMAM, potentially hindering the drug from proteolytic degradation and enabling its release at a membrane level. Viability experiments on HeLa, PC‐12, and HEK‐293 cells incubated with increasing concentrations of octreotide in free drug solutions and equimolar mixtures with PEG‐PAMAM confirmed that the PEGylated dendrimer acts as an efficient supramolecular carrier for octreotide and enhances the antiproliferative effects of the drug. Our findings highlight a novel facet for PEG‐PAMAM dendrimers as macromolecular vehicles for peptide or non‐peptide drugs acting via membrane receptor sites.

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Enhancement of octreotide antiproliferative activity by PEGylated PAMAM dendrimers delivery

Díaz,

Cifuentes,

Oyarzún

et al. 2024

J of Applied Polymer Sci

Self Cite

View full text Add to dashboard Cite

show abstract

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Cell internalization kinetics and surface charge accessibility of surface-modified PAMAM dendrimers

Abstract: The accessibility of surface cationic charges is a key determinant for the cell internalization capacity of surface-modified PAMAM dendrimers with acetyl, folate or poly(ethylene glycol) groups.

Cited by 1 publication

References 49 publications

Enhancement of octreotide antiproliferative activity by PEGylated PAMAM dendrimers delivery

Enhancement of octreotide antiproliferative activity by PEGylated PAMAM dendrimers delivery

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