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-  2019 

Oligopeptide-side chained alginate nanocarrier for melittin-targeted chemotherapy

DOI: https://doi.org/10.1038/s41428-019-0191-6

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Abstract:

A melittin-targeting drug carrier was successfully synthesized by the grafting of sodium alginate to an oligopeptide via an amidation method at different oligopeptide:alginate unit molar ratios. The average sizes of the oligopeptide–alginate nanoparticles formed in the presence of 1?mM CaCl2 decreased with increasing oligopeptide contents, indicating intramolecular interactions between oligopeptide-side chains. While the doxorubicin-loading efficiency on nanoparticles (0.1:1) was similar to that of alginate nanoparticles, the melittin-loading onto oligopeptide–alginate nanoparticles (0.1:1) was more than double that onto alginate nanoparticles, suggesting the specific interaction of melittin with the oligopeptide-side chain in the oligopeptide–alginate nanoparticles. While 2.5?μM free melittin caused almost no damage to Caco-2 cells, more than 80% of cells did not survive under the dose of 2.5?μM melittin-loaded oligopeptide–alginate nanoparticles. The results confirm that the derivation of an oligopeptide-side chain in alginate offers a specific binding site for melittin and effectively works in cancer chemotherapy

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