title: Core-shell biodegradable nanoassemblies for the passive targeting of docetaxel: features, antiproliferative activity and in vivo toxicity.
abstract: Amphiphilic block copolymers of poly(ɛ-caprolactone) and poly(ethylene oxide) were assembled in core-shell nanoparticles (NPs) by a melting-sonication technique (MeSo). The entrapment of the poorly water-soluble anticancer drug docetaxel (DTX), nanocarrier cytotoxicity toward different cells and toxicity in mice were investigated. The encapsulation mechanism was rationalized and related to copolymer properties such as crystallinity and drug solubility in the copolymer phase. DTX release from NPs occurred in 2 drug pulses over 30 days. DTX entrapment in NPs strongly decreased haemolysis of erythrocytes in comparison with a commercial DTX formulation. In comparison with free DTX, NPs were both more efficient in inhibiting cell growth of breast and prostate cancer cells and less toxic in experimental animal models. The results of this study indicate that MeSo is an interesting technique for the achievement of peculiar core-shell nanocarriers for the passive targeting and sustained release of poorly water-soluble anticancer drugs.
  
  
  BACKGROUND
  In this study, stealth nanoparticles of PEO/PCL block copolymers for passive targeting of docetaxel to solid tumors were developed using a novel technique. The studied properties of NPs suggest strong potential as anticancer drug-delivery system.
authors: Department of Pharmaceutical and Toxicological Chemistry, University of Naples Federico II, Naples, Italy.
authors: Francesca
authors: F
authors: Ungaro
authors: Claudia
authors: C
authors: Conte
authors: Luisanna
authors: L
authors: Ostacolo
authors: Giovanni
authors: G
authors: Maglio
authors: Antonio
authors: A
authors: Barbieri
authors: Claudio
authors: C
authors: Arra
authors: Gabriella
authors: G
authors: Misso
authors: Alberto
authors: A
authors: Abbruzzese
authors: Michele
authors: M
authors: Caraglia
authors: Fabiana
authors: F
authors: Quaglia
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000009:adverse effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation; D000077143:Docetaxel; D016503:Drug Delivery Systems / Q000009:adverse effects / Q000379:methods; D004912:Erythrocytes / Q000187:drug effects; D005615:Freezing; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry; D011091:Polyesters / Q000008:administration & dosage / Q000737:chemistry; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000737:chemistry; D013010:Sonication / Q000379:methods; D043823:Taxoids / Q000008:administration & dosage / Q000009:adverse effects
chemical_list: D000970:Antineoplastic Agents; D011091:Polyesters; D043823:Taxoids; D000077143:Docetaxel; C016240:polycaprolactone; D011092:Polyethylene Glycols