title: Lipid-core nanocapsules as a nanomedicine for parenteral administration of tretinoin: development and in vitro antitumor activity on human myeloid leukaemia cells.
abstract: Tretinoin-loaded conventional nanocapsules have showed a significant protection of this drug against UVC radiation. However, this formulation presents a limited stability on storage. We hypothesized that the association of tretinoin to lipid-core nanocapsules could increase the physicochemical stability of such formulations, focusing on the development of a reliable nanomedicine for parenteral administration. However, this advantage should still be accompanied by the known photoprotective effect of conventional polymeric nanocapsules against the exposure of tretinoin to UV radiation. Results showed that tretinoin-loaded lipid-core nanocapsules improved the physicochemical stability of formulations under storage, without changing their ability to protect tretinoin either against UVA or UVC radiation. In addition, the effect of nanoencapsulation on the antiproliferative and differentiation properties of tretinoin was studied on human myeloid leukemia cells (HL60 cells) showing that tretinoin-loaded lipid-core nanocapsules presents a longer antitumor efficiency compared to the free tretinoin. These results allow us to propose the current formulation (tretinoin-loaded lipid-core nanocapsules) as a promising parenteral nanomedicine for the treatment of acute promyelocytic leukaemia.
authors.affiliation: Curso de Farmácia, Centro de Ciências da Saúde, Universidade Federal de Santa Maria (UFSM), Av. Roraima, 1000, 97105-900 Santa Maria, RS, Brazil.
authors.forename: A F
authors.initials: AF
authors.lastname: Ourique
authors.forename: S
authors.initials: S
authors.lastname: Azoubel
authors.forename: C V
authors.initials: CV
authors.lastname: Ferreira
authors.forename: C B
authors.initials: CB
authors.lastname: Silva
authors.forename: M C L
authors.initials: MC
authors.lastname: Marchiori
authors.forename: A R
authors.initials: AR
authors.lastname: Pohlmann
authors.forename: S S
authors.initials: SS
authors.lastname: Guterres
authors.forename: R C R
authors.initials: RC
authors.lastname: Beck
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry; D002470:Cell Survival / Q000187:drug effects*; D004339:Drug Compounding / Q000379:methods; D004355:Drug Stability; D018922:HL-60 Cells; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D053769:Nanocapsules / Q000008:administration & dosage* / Q000737:chemistry*; D014212:Tretinoin / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D008055:Lipids; D053769:Nanocapsules; D014212:Tretinoin