Supramolecular Fmoc-valyl based nanoassemblies for delivery of mitoxantrone into HeLa cells

Recent advances in nanotechnology have allowed for engineering efficient nanoparticulate drug delivery vehicles for the controlled release of therapeutic drugs. Herein, we have developed a new nanoscale drug delivery system formed by the conjugation of fluorenylmethyloxycarbonyl (Fmoc)-valine with N1,N5 Bis-Boc spermidine (boc-spermidine), which spontaneously self-assembled into supramolecular nanoassemblies under aqueous conditions. To explore the efficiency of the nanoassemblies as a drug delivery vehicle, we incorporated the antineoplastic drug Mitoxantrone. FTIR spectroscopy and differential scanning calorimetry were utilized to study the interactions involved between the nanoassemblies and the drug. The incorporation of the drug was also confirmed by electron microscopy. The encapsulation efficiency was found to be dependent upon the concentration of the drug utilized. In vitro release profiles indicated that the nanoassemblies exhibited sustained release of the drug over a period of 240 h. Furthermore, the nanoassemblies were biocompatible with mammalian (HeLa) tumorigenic cells, but could release encapsulated Mitoxantrone into these cells and lead to cell death. Thus we have devised a novel nanoparticulate drug delivery system with potential applications as a chemotherapeutic delivery agent.

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