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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Cited by 3 publications

References 49 publications

(76 reference statements)

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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

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Fine-Tuned “Click” Functionalization of PAMAM Dendrimers with a Linear Fluorinated Guanidino Linker: Synthesis, Characterization, and Applications

Romani,

Gagni,

Di Pietro

et al. 2024

Bioconjugate Chem.

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Gallic Acid-Encapsulated PAMAM Dendrimers as an Antioxidant Delivery System for Controlled Release and Reduced Cytotoxicity against ARPE-19 Cells

Sripunya,

Chittasupho,

Mangmool

et al. 2024

Bioconjugate Chem.

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Poly(amidoamine) (PAMAM) dendrimers have gained significant attention in various research fields, particularly in medicinal compound delivery. Their versatility lies in their ability to conjugate with functional molecules on their surfaces and encapsulate small molecules, making them suitable for diverse applications. Gallic acid is a potent antioxidant compound that has garnered considerable interest in recent years. Our research aims to investigate if the gallic acid-encapsulated PAMAM dendrimer generations 4 (G4(OH)-Ga) and 5 (G5(OH)-Ga) could enhance radical scavenging, which could potentially slow down the progression of age-related macular degeneration (AMD). Encapsulation of gallic acid in PAMAM dendrimers is a feasible alternative to prevent its degradation and toxicity. In vitro investigation of antioxidant activity was carried out using the DPPH and ABTS radical scavenging assays, as well as the FRAP assay. The IC 50 values for DPPH and ABTS assays were determined through nonlinear dose−response curves, correlating the inhibition percentage with the concentration (μg/mL) of the sample and the concentration (μM) of gallic acid within each sample. G4(OH)-Ga and G5(OH)-Ga possess significant antioxidant activities as determined by the DPPH, ABTS, and FRAP assays. Moreover, gallic acid-encapsulated PAMAM dendrimers inhibit H 2 O 2 -induced reactive oxygen species (ROS) production in the human retinal pigment epithelium ARPE-19 cells, thereby improving antioxidant characteristics and potentially retarding AMD progression caused by ROS. In an evaluation of cell viability of ARPE-19 cells using the MTT assay, G4(OH)-Ga was found to reduce cytotoxic effects on ARPE-19 cells.

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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 3 publications

References 49 publications

Enhancement of octreotide antiproliferative activity by PEGylated PAMAM dendrimers delivery

Enhancement of octreotide antiproliferative activity by PEGylated PAMAM dendrimers delivery

Fine-Tuned “Click” Functionalization of PAMAM Dendrimers with a Linear Fluorinated Guanidino Linker: Synthesis, Characterization, and Applications

Gallic Acid-Encapsulated PAMAM Dendrimers as an Antioxidant Delivery System for Controlled Release and Reduced Cytotoxicity against ARPE-19 Cells

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