2. Academic Validation
  3. New class of squalene-based releasable nanoassemblies of paclitaxel, podophyllotoxin, camptothecin and epothilone A

New class of squalene-based releasable nanoassemblies of paclitaxel, podophyllotoxin, camptothecin and epothilone A

  • Eur J Med Chem. 2014 Oct 6:85:179-90. doi: 10.1016/j.ejmech.2014.07.035.
Stella Borrelli 1,  Michael S Christodoulou 1,  Ilaria Ficarra 1,  Alessandra Silvani 1,  Graziella Cappelletti 2,  Daniele Cartelli 2,  Giovanna Damia 3,  Francesca Ricci 3,  Massimo Zucchetti 3,  Franco Dosio 4,  Daniele Passarella 5
Affiliations

Affiliations

  • 1 Dipartimento di Chimica, Università degli Studi di Milano, Via C. Golgi 19, 20133 Milano, Italy.
  • 2 Dipartimento di Bioscienze, Università degli Studi di Milano, Via Celoria 26, 20133 Milano, Italy.
  • 3 Department of Oncology, IRCCS-Istituto di Ricerche Farmacologiche Mario Negri, Via La Masa 19, 20156 Milano, Italy.
  • 4 Dipartimento di Scienza e Tecnologia del Farmaco, Via Giuria 9, 10125 Torino, Italy.
  • 5 Dipartimento di Chimica, Università degli Studi di Milano, Via C. Golgi 19, 20133 Milano, Italy. Electronic address: daniele.passarella@unimi.it.
PMID: 25084144 DOI: 10.1016/j.ejmech.2014.07.035
Abstract

The present study reports the preparation of a novel class of squalene conjugates with paclitaxel, podophyllotoxin, camptothecin and epothilone A. The obtained compounds are characterized by a squalene tail that makes them able to self-assemble in water, and by a drug unit connected via a disulfide-containing linker to secure the release inside the cell. All the obtained compounds were effectively able to self-assemble and to release the parent drug in vitro. Disulfide-containing paclitaxel-squalene derivative showed a similar biological activity when compared to the free drug. Immunofluorescence assay shows that this squalene conjugate enters A549 cells and stain microtubule bundles. The results described herein pave the way for different classes of squalene-based releasable nanoassemblies.

Keywords

Camptothecin; Epothilone A; Nanoassemblies; Paclitaxel; Podophyllotoxin; Squalene derivatives.

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