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.
Readily prepared biodegradable nanoparticles to formulate poorly water soluble drugs improving their pharmacological properties : the example of trabectedin / U. Capasso Palmiero, L. Morosi, E. Bello, M. Ponzo, R. Frapolli, C. Matteo, M. Ferrari, M. Zucchetti, L. Minoli, M. De Maglie, P. Romanelli, M. Morbidelli, M. D'Incalci, D. Moscatelli. - In: JOURNAL OF CONTROLLED RELEASE. - ISSN 0168-3659. - 276(2018), pp. 140-149.
|Titolo:||Readily prepared biodegradable nanoparticles to formulate poorly water soluble drugs improving their pharmacological properties : the example of trabectedin|
|Parole Chiave:||Biodegradable; Nanoparticles; Phlebitis; Polycaprolactone; Polyethylen glycol; Trabectedin; Vascular toxicity; Animals; Female; Liposarcoma; Mice, Inbred C57BL; Mice, Nude; Polymers; Skin; Solubility; Tissue Distribution; Water; Antineoplastic Agents, Alkylating; Nanoparticles; Trabectedin|
|Settore Scientifico Disciplinare:||Settore VET/03 - Patologia Generale e Anatomia Patologica Veterinaria|
|Data di pubblicazione:||2018|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1016/j.jconrel.2018.03.005|
|Appare nelle tipologie:||01 - Articolo su periodico|