Readily prepared biodegradable nanoparticles to formulate poorly water soluble drugs improving their pharmacological properties: The example of trabectedin

Umberto Capasso Palmiero, Lavinia Morosi, Ezia Bello, Marianna Ponzo, Roberta Frapolli, Cristina Matteo, Mariella Ferrari, Massimo Zucchetti, Lucia Minoli, Marcella De Maglie, Pierpaolo Romanelli, Massimo Morbidelli, Maurizio D'Incalci, Davide Moscatelli

Research output: Contribution to journalArticle

Abstract

The improvement of the pharmacological profile of lipophilic drug formulations is one of the main successes achieved using nanoparticles (NPs) in medicine. However, the complex synthesis procedure and numerous post-processing steps hamper the cost-effective use of these formulations. In this work, an approach which requires only a syringe to produce self-assembling biodegradable and biocompatible poly(caprolactone)-based NPs is developed. The effective synthesis of monodisperse NPs has been made possible by the optimization of the block-copolymer synthesized via a combination of ring opening polymerization and reversible addition-fragmentation chain transfer polymerization. These NPs can be used to formulate lipophilic drugs that are barely soluble in water, such as trabectedin, a potent anticancer therapeutic. Its biodistribution and antitumor activity have been compared with the commercially available formulation Yondelis®. The results indicate that this trabectedin NP formulation performs with the same antitumor activity as Yondelis®, but does not have the drawback of severe local vascular toxicity in the injection site.

Original languageEnglish
Pages (from-to)140-149
Number of pages10
JournalJournal of Controlled Release
Volume276
DOIs
Publication statusPublished - Apr 28 2018

Keywords

  • Biodegradable
  • Nanoparticles
  • Phlebitis
  • Polycaprolactone
  • Polyethylen glycol
  • Trabectedin
  • Vascular toxicity

ASJC Scopus subject areas

  • Pharmaceutical Science

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