title: In vitro and in vivo effects of free and chalcones-loaded nanoemulsions: insights and challenges in targeted cancer chemotherapies.
abstract: Several obstacles are encountered in conventional chemotherapy, such as drug toxicity and poor stability. Nanotechnology is envisioned as a strategy to overcome these effects and to improve anticancer therapy. Nanoemulsions comprise submicron emulsions composed of biocompatible lipids, and present a large surface area revealing interesting physical properties. Chalcones are flavonoid precursors, and have been studied as cytotoxic drugs for leukemia cells that induce cell death by different apoptosis pathways. In this study, we encapsulated chalcones in a nanoemulsion and compared their effect with the respective free compounds in leukemia and in non-tumoral cell lines, as well as in an in vivo model. Free and loaded-nanoemulsion chalcones induced a similar anti-leukemic effect. Free chalcones induced higher toxicity in VERO cells than chalcones-loaded nanoemulsions. Similar results were observed in vivo. Free chalcones induced a reduction in weight gain and liver injuries, evidenced by oxidative stress, as well as an inflammatory response. Considering the high toxicity and the side effects induced generally by all cancer chemotherapies, nanotechnology provides some options for improving patients' life quality and/or increasing survival rates.
authors.affiliation: Department of Pharmaceutical Sciences, Federal University of Santa Catarina, P.O. Box 476, Florianópolis, SC 88040-900, Brazil. eve_winter@hotmail.com.
authors.forename: Evelyn
authors.initials: E
authors.lastname: Winter
authors.affiliation: Department of Pharmaceutical Sciences, Federal University of Santa Catarina, P.O. Box 476, Florianópolis, SC 88040-900, Brazil. carinedp@gmail.com.
authors.forename: Carine Dal
authors.initials: CD
authors.lastname: Pizzol
authors.affiliation: Department of Pharmacy, University of West of Santa Catarina, Videira, SC 89560-000, Brazil. claudrilocatelli@gmail.com.
authors.forename: Claudriana
authors.initials: C
authors.lastname: Locatelli
authors.affiliation: Department of Pharmaceutical Sciences, Federal University of Santa Catarina, P.O. Box 476, Florianópolis, SC 88040-900, Brazil. adnyh@yahoo.com.br.
authors.forename: Adny H
authors.initials: AH
authors.lastname: Silva
authors.affiliation: Department of Pharmacy, University of West of Santa Catarina, Videira, SC 89560-000, Brazil. alineconte91@gmail.com.
authors.forename: Aline
authors.initials: A
authors.lastname: Conte
authors.affiliation: Department of Chemistry, Federal University of Santa Catarina, P.O. Box 476, Florianópolis, SC 88040-900, Brazil.
authors.forename: Louise D
authors.initials: LD
authors.lastname: Chiaradia-Delatorre
authors.affiliation: Department of Chemistry, Federal University of Santa Catarina, P.O. Box 476, Florianópolis, SC 88040-900, Brazil. nunesricardoj@gmail.com.
authors.forename: Ricardo J
authors.initials: RJ
authors.lastname: Nunes
authors.affiliation: Department of Chemistry, Federal University of Santa Catarina, P.O. Box 476, Florianópolis, SC 88040-900, Brazil. ryunes@msn.com.
authors.forename: Rosendo A
authors.initials: RA
authors.lastname: Yunes
authors.affiliation: Department of Pharmaceutical Sciences, Federal University of Santa Catarina, P.O. Box 476, Florianópolis, SC 88040-900, Brazil. tania.pasa@ufsc.br.
authors.forename: Tânia B
authors.initials: TB
authors.lastname: Creckzynski-Pasa
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000633:toxicity*; D047188:Chalcones / Q000008:administration & dosage / Q000633:toxicity*; D002522:Chlorocebus aethiops; D016503:Drug Delivery Systems / Q000379:methods; D004655:Emulsions / Q000008:administration & dosage / Q000737:chemistry*; D066298:In Vitro Techniques; D007938:Leukemia / Q000188:drug therapy*; D007939:Leukemia L1210; D008099:Liver / Q000473:pathology; D008297:Male; D051379:Mice; D058990:Molecular Targeted Therapy; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry; D018384:Oxidative Stress; D014709:Vero Cells
chemical_list: D000970:Antineoplastic Agents; D047188:Chalcones; D004655:Emulsions