Self-assembly of Amphiphilic Tripeptides into Nanoparticles for Drug Delivery

Zhaoxu      Tu; Xianghui      Xu; Yeting      Jian; Dan      Zhong; Bin      He; Zhongwei      Gu

doi:10.2174/09298665113206660117

Abstract

Peptide-based nanomaterials are widely used as nanocarriers for catalysis, drug delivery, and gene delivery. In this paper, we designed and synthesized the amphiphilic tripeptides through solution phase synthesis. The tripeptides were purified by column chromatography and the molecular structures were confirmed by ¹H NMR and TOF-MS. The tripeptides could self-assemble into spherical nanoparticles in aqueous media with a low critical aggregation concentration. The size and morphology of the nanoparticles were performed by dynamic light scattering, scanning electron microscopy and transmission electron microscope. The peptide-based nanoparticles were used as biocompatible nanocarriers for encapsulating hydrophobic doxorubicin (DOX) to achieve controlled release. The CCK-8 assay indicated that the peptide-based nanocarriers could enhance cellular uptake and drug efficacy of DOX to A549 tumor cell line. These results showed that the self-assembly of amphiphilic tripeptides provided a facile strategy to fabricate nanoparticles for anti-tumor drug delivery.

Keywords: Amphiphilic tripeptide, controlled release, cytotoxicity, drug delivery, nanoparticles, self-assembly.

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