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Stearylated cycloarginine nanosystems for intracellular delivery - simulations, formulation and proof of concept
Cationization of nanocarriers has been sought after as a viable strategy to surmount cellular barriers that impede intracellular drug and gene delivery. A plethora of cationic compounds including both lipids and polymers have been designed and developed for efficient cellular penetration. The toxici...
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Published in: | RSC advances 2016-01, Vol.6 (114), p.113538-11355 |
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Main Authors: | , , , , , , , , , , , |
Format: | Article |
Language: | English |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
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Summary: | Cationization of nanocarriers has been sought after as a viable strategy to surmount cellular barriers that impede intracellular drug and gene delivery. A plethora of cationic compounds including both lipids and polymers have been designed and developed for efficient cellular penetration. The toxicity of these cationic agents, however, precludes their use in drug delivery. Conjugation with biomolecules like sugars and amino acids to produce novel cationic agents is being investigated to generate biocompatible molecules to achieve safe drug delivery. In this study, we propose to mitigate the toxicity of stearylamine, a cationic lipid, by tethering it to arginine, to yield a novel cationic ligand. Ligand loaded liposomes and nanoparticles were fabricated and evaluated for their surface charge and cellular uptake. Furthermore, molecular dynamics simulations were utilized as a tool to understand the accessibility of the novel ligand and stearylamine loaded liposomal systems. This paper presents the one pot synthesis of a novel stearylated arginine dipeptide and its incorporation in delivery systems along with its
in vitro
and
in vivo
toxicity evaluation.
Novel cationic agent liposomes performed better
in silico
translating in higher cellular uptake with reduced toxicity. |
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ISSN: | 2046-2069 2046-2069 |
DOI: | 10.1039/c6ra16432c |