title: Antitumor activity of PEGylated biodegradable nanoparticles for sustained release of docetaxel in triple-negative breast cancer.
abstract: With the aim to find novel therapeutical approaches for triple-negative breast cancer (TNBC) treatment, we have developed a powder for i.v. injection based on cyclodextrins and docetaxel (DTX)-loaded polyethyleneglycol-poly(epsilon-caprolactone) nanoparticles (DTX-NPs). Nanoparticles are designed to concentrate at tumor level by enhanced permeability and retention effect and release drug cargo at a sustained rate in the blood and in tumor interstitium. DTX-NPs of around 70 nm, shielding proteins and allowing a sustained DTX release for about 30 days, were produced by melting sonication technique. DTX-NPs were associated to hydroxypropyl-β-cyclodextrin to give a powder for injection with excellent dispersibility and suitable for i.v. administration. DTX-NPs were as efficient as free DTX in inhibiting cell growth of MDA-MB231 cells, even at low concentrations, and displayed a comparable in vivo antitumor efficacy and better survival in a TNBC animal model as compared with DTX commercial formulation (Taxotere(®)). In conclusion, PEGylated biodegradable DTX-NPs highlighted their potential in the treatment of aggressive TNBC providing a foundation for future clinical studies.
authors.affiliation: Animal Facility, National Cancer Institute - Foundation "G. Pascale", Via Mariano Semmola, 80131 Napoli, Italy; Institute of Experimental Endocrinology and Oncology, CNR, Via Pansini, 80131 Napoli, Italy.
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Palma
authors.affiliation: Drug Delivery Laboratory, Department of Pharmacy, University of Napoli Federico II, Via Domenico Montesano 49, 80131 Napoli, Italy.
authors.forename: Claudia
authors.initials: C
authors.lastname: Conte
authors.affiliation: Animal Facility, National Cancer Institute - Foundation "G. Pascale", Via Mariano Semmola, 80131 Napoli, Italy.
authors.forename: Antonio
authors.initials: A
authors.lastname: Barbieri
authors.affiliation: Animal Facility, National Cancer Institute - Foundation "G. Pascale", Via Mariano Semmola, 80131 Napoli, Italy.
authors.forename: Sabrina
authors.initials: S
authors.lastname: Bimonte
authors.affiliation: Animal Facility, National Cancer Institute - Foundation "G. Pascale", Via Mariano Semmola, 80131 Napoli, Italy.
authors.forename: Antonio
authors.initials: A
authors.lastname: Luciano
authors.affiliation: Animal Facility, National Cancer Institute - Foundation "G. Pascale", Via Mariano Semmola, 80131 Napoli, Italy.
authors.forename: Domenica
authors.initials: D
authors.lastname: Rea
authors.affiliation: Drug Delivery Laboratory, Department of Pharmacy, University of Napoli Federico II, Via Domenico Montesano 49, 80131 Napoli, Italy.
authors.forename: Francesca
authors.initials: F
authors.lastname: Ungaro
authors.affiliation: Department of Chemistry Paolo Corradini, University of Napoli Federico II, Via Cintia, 80126 Napoli, Italy.
authors.forename: Pasquale
authors.initials: P
authors.lastname: Tirino
authors.affiliation: Drug Delivery Laboratory, Department of Pharmacy, University of Napoli Federico II, Via Domenico Montesano 49, 80131 Napoli, Italy. Electronic address: quaglia@unina.it.
authors.forename: Fabiana
authors.initials: F
authors.lastname: Quaglia
authors.affiliation: Animal Facility, National Cancer Institute - Foundation "G. Pascale", Via Mariano Semmola, 80131 Napoli, Italy.
authors.forename: Claudio
authors.initials: C
authors.lastname: Arra
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry; D001798:Blood Proteins / Q000737:chemistry; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry; D000077143:Docetaxel; D005026:Ethylene Glycols / Q000737:chemistry*; D005260:Female; D006801:Humans; D008325:Mammary Neoplasms, Experimental / Q000188:drug therapy* / Q000473:pathology; D008819:Mice, Nude; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D011091:Polyesters / Q000737:chemistry*; D011208:Powders; D043823:Taxoids / Q000008:administration & dosage* / Q000737:chemistry; D064726:Triple Negative Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D047368:Tumor Burden / Q000187:drug effects; D047392:beta-Cyclodextrins / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D001798:Blood Proteins; D003692:Delayed-Action Preparations; D005026:Ethylene Glycols; D011091:Polyesters; D011208:Powders; D043823:Taxoids; D047392:beta-Cyclodextrins; C476300:poly(epsilon-caprolactone)-b-poly(ethylene glycol); D000077143:Docetaxel; D000073738:2-Hydroxypropyl-beta-cyclodextrin
keywords: Docetaxel; PEGylated nanoparticles; Powder for injection; Sustained release; Triple-negative breast cancer