Self-assembled micelles of the (lipo) glycopeptides, teicoplanin, as taxane nanocarriers

COMINI, LAURA RAQUEL; ALASINO, ROXANA VALERIA; LEONHARD, VICTORIA; BIERBRAUER, KARINA LILIAN; BELTRAMO, DANTE MIGUEL

NANOTECHNOLOGY

IOP PUBLISHING LTD

Año: 2021 vol. 32

0957-4484

The use of nanoparticles is one of the strategies currently studied to minimize the toxicity andlack of tissue specificity of many cancer drugs used in chemotherapy. In this research thephysicochemical and biological behavior of a novel self-assembled nanostructure of theantibiotic Teicoplanin (Teico) was characterized as a nanocarrier system for solubilizing highlyhydrophobic drugs like Paclitaxel (Ptx) in aqueous media. The Teico micelles were loaded withPtx in DMSO or PEG-400. The interaction between the loaded micelles and Albumin humanserum albumin (HSA) was then studied by size exclusion chromatography. Transmissionelectron microscopy, dynamic light scattering and high-resolution liquid chromatography werealso used to characterize the physicochemical and structural properties of the micelles to form theTeico/Ptx and Teico/Ptx/HSA micelles. Cellular uptake of Ptx was evaluated by fluorescentmicroscopy. The in vitro cytotoxicity of the complexes was studied on Hep-2 tumor cells, by aCrystal Violet assay. Teico cosolvent-free micelles can solubilize up to 20 mg.ml−1 of Ptxdissolved in PEG, increasing four times the solubility of Ptx in water compared to Abraxane, and20 000 times the intrinsic solubility of Ptx in water. In addition, Teico/Ptx micelles bindsspontaneously HSA through hydrophobic interaction. Teico and Teico/HSA micelles as a Ptxtransporter does not affect its release or biological activity. Therefore, Teico/Ptx or Teico/Ptx/HSA complexes appear as new alternatives for transporting larger amounts of hydrophobic drugsthat offer advantages, turning it an interesting option for further study.