title: Enhanced Efficacy of Artemisinin Loaded in Transferrin-Conjugated Liposomes versus Stealth Liposomes against HCT-8 Colon Cancer Cells.
abstract: Artemisinin (ART) is a unique sesquiterpene lactone isolated from Artemisia annua that is well known for antimalarial properties and was recently reported as a promising anticancer drug. The aim of our work was to develop a novel nanocarrier for enhanced ART delivery and activation in cancer tissues, because transferrin receptors are largely expressed in cancer cells and the iron content is higher than in normal cells. ART was loaded in transferrin-conjugated liposomes (ART-L-Tf), and the performance was compared with ART loaded in stealth liposomes (ART-L). All of the liposomes were fully characterized in terms of size, drug-entrapment efficiency, transferrin coupling moieties, and stability. Both cell uptake and cytotoxicity studies of the developed nanocarriers were tested in the HCT-8 cell line, selected among several cell lines because of transferrin receptor overexpression. The results confirmed the enhanced delivery of ART-L-Tf in comparison with ART-L in the targeting of the HCT-8 cell line and an improved cytotoxicity as a result of the presence of iron ions, which resulted in concomitant synergism derived from the increased expression of transferrin receptors on the surface of the tumor cells.
authors.affiliation: Department of Chemistry, University of Florence, via U. Schiff 6, 50019, Sesto Fiorentino, Florence, Italy.
authors.forename: Isabella
authors.initials: I
authors.lastname: Leto
authors.affiliation: Department of Health Sciences, Clinical Pharmacology and Oncology Section, University of Florence, viale Pieraccini 6, 50139, Florence, Italy.
authors.forename: Marcella
authors.initials: M
authors.lastname: Coronnello
authors.affiliation: Department of Chemistry, University of Florence, via U. Schiff 6, 50019, Sesto Fiorentino, Florence, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Righeschi
authors.affiliation: Department of Chemistry, University of Florence, via U. Schiff 6, 50019, Sesto Fiorentino, Florence, Italy.
authors.forename: Maria Camilla
authors.initials: MC
authors.lastname: Bergonzi
authors.affiliation: Department of Health Sciences, Clinical Pharmacology and Oncology Section, University of Florence, viale Pieraccini 6, 50139, Florence, Italy.
authors.forename: Enrico
authors.initials: E
authors.lastname: Mini
authors.affiliation: Department of Chemistry, University of Florence, via U. Schiff 6, 50019, Sesto Fiorentino, Florence, Italy. ar.bilia@unifi.it.
authors.forename: Anna Rita
authors.identifier: 0000-0001-8772-1895
authors.initials: AR
authors.lastname: Bilia
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology*; D037621:Artemisinins / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D003110:Colonic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry*; D006801:Humans; D008081:Liposomes; D015394:Molecular Structure; D011990:Receptors, Transferrin / Q000096:biosynthesis; D013329:Structure-Activity Relationship; D014168:Transferrin / Q000008:administration & dosage* / Q000737:chemistry*; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D037621:Artemisinins; D004337:Drug Carriers; D008081:Liposomes; D011990:Receptors, Transferrin; D014168:Transferrin; C031327:artemisinin
keywords: antitumor agents; artemisinin; cell recognition; drug delivery; liposomes