title: Transferrin-conjugated pluronic niosomes as a new drug delivery system for anticancer therapy.
abstract: An efficient tumor-targeted niosomal delivery system for the vehiculation of doxorubicin hydrochloride as an anticancer agent was designed. Niosomes were prepared from a mixture of an opportunely modified Pluronic L64 surfactant and cholesterol as a membrane additive and characterized in terms of size and related distribution function and drug entrapment efficiency. After the preparation, transferrin was conjugated to niosomes to produce transferrin (Tf) niosomes, and the cytotoxicity of the final formulation was studied. The specific uptake of Tf niosomes into cells was evaluated via incubation of MCF-7 and MDA-MB-231 cells with fluorescently rhodamine-loaded Tf niosomes for various times and concentration intervals and further investigated by fluorescence microscopy. Results showed that doxorubicin can be easily encapsulated into niosomes, which are regular and spherical in shape. Moreover, transferrin conjugate niosomes demonstrated far greater extents of cellular uptake by MCF-7 and MDA-MB-231 cells, suggesting that they were mainly taken up by transferrin receptor-mediated endocytosis. Doxorubicin-loaded niosome anticancer activity was also achieved against MCF-7 and MDA-MB-231 tumor cell lines, and a significant reduction in viability in a dose- and time-related manner was observed. Finally, our formulation could be potentially useful as a target doxorubicin delivery system in anticancer therapy.
authors.affiliation: Dipartimento di Farmacia e Scienze della Salute e della Nutrizione, Università della Calabria , Edificio Polifunzionale, 87036 Arcavacata di Rende, Cosenza, Italy.
authors.forename: Lorena
authors.initials: L
authors.lastname: Tavano
authors.forename: Rita
authors.initials: R
authors.lastname: Muzzalupo
authors.forename: Loredana
authors.initials: L
authors.lastname: Mauro
authors.forename: Michele
authors.initials: M
authors.lastname: Pellegrino
authors.forename: Sebastiano
authors.initials: S
authors.lastname: Andò
authors.forename: Nevio
authors.initials: N
authors.lastname: Picci
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D016503:Drug Delivery Systems / Q000379:methods*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008081:Liposomes; D061986:MCF-7 Cells; D008958:Models, Molecular; D015394:Molecular Structure; D020442:Poloxamer / Q000008:administration & dosage / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014168:Transferrin / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D008081:Liposomes; D014168:Transferrin; D020442:Poloxamer; D004317:Doxorubicin; C514452:pluronic L64