Renata S Fernandes1, Juliana O Silva1, Samuel V Mussi1, Sávia C A Lopes1, Elaine A Leite1, Geovanni D Cassali2, Valbert N Cardoso1, Danyelle M Townsend3, Patrick M Colletti4, Lucas A M Ferreira1, Domenico Rubello5, André L B de Barros6. 1. Faculty of Pharmacy, Universidade Federal de Minas Gerais, Av. Antônio Carlos, 6627, Belo Horizonte, Minas Gerais, 31270-901, Brazil. 2. Biological Science Institute, Universidade Federal de Minas Gerais, Av. Antônio Carlos, 6627, Belo Horizonte, Minas Gerais, 31270-901, Brazil. 3. Department of Drug Discovery and Experimental Therapeutics, Medical University of South Carolina, Charleston, SC, USA. 4. Department of Radiology, University of Southern California, Los Angeles, CA, USA. 5. Department of Nuclear Medicine, Radiology, NeuroRadiology, Medical Physics, Clinical Pathology & Molecular Biology, Santa Maria della Misericordia Hospital, Via Tre Martiri, 140, 45100, Rovigo, Italy. domenico.rubello@libero.it. 6. Faculty of Pharmacy, Universidade Federal de Minas Gerais, Av. Antônio Carlos, 6627, Belo Horizonte, Minas Gerais, 31270-901, Brazil. brancodebarros@yahoo.com.br.
Abstract
PURPOSE: Nanotheranostic platforms, i.e., the combination of both therapeutic and diagnostic agents on a single platform, are emerging as an interesting tool for the personalized cancer medicine. Therefore, the aim of this work was to evaluate the in vivo properties of a Tc-99m-labeled nanostructured lipid carrier (NLC) formulation, co-loaded with doxorubicin (DOX) and docosahexaenoic acid (DHA), for theranostic applications. PROCEDURES: NLC-DHA-DOX were prepared busing the hot melting homogenization method using an emulsification-ultrasound and were radiolabeled with Tc-99m. Biodistribution studies, scintigraphic images, and antitumor activity were performed in 4T1 tumor-bearing mice. RESULTS: NCL was successfully radiolabeled with Tc-99m. Blood clearance showed a relatively long half-life, with blood levels decaying in a biphasic manner (T1/2 α = 38.7 min; T1/2 β = 516.5 min). The biodistribution profile and scintigraphic images showed higher tumor uptake compared to contralateral muscle in all time-points investigated. Antitumor activity studies showed a substantial tumor growth inhibition ratio for NLC-DHA-DOX formulation. In addition, the formulation showed more favorable toxicity profiles when compared to equivalent doses of free administered drugs, being able to reduce heart and liver damage. CONCLUSIONS: Therefore, NLC-DHA-DOX formulation demonstrated feasibility in breast cancer treatment and diagnosis/monitoring, leading to a new possibility of a theranostic platform.
PURPOSE: Nanotheranostic platforms, i.e., the combination of both therapeutic and diagnostic agents on a single platform, are emerging as an interesting tool for the personalized cancer medicine. Therefore, the aim of this work was to evaluate the in vivo properties of a Tc-99m-labeled nanostructured lipid carrier (NLC) formulation, co-loaded with doxorubicin (DOX) and docosahexaenoic acid (DHA), for theranostic applications. PROCEDURES: NLC-DHA-DOX were prepared busing the hot melting homogenization method using an emulsification-ultrasound and were radiolabeled with Tc-99m. Biodistribution studies, scintigraphic images, and antitumor activity were performed in 4T1 tumor-bearing mice. RESULTS:NCL was successfully radiolabeled with Tc-99m. Blood clearance showed a relatively long half-life, with blood levels decaying in a biphasic manner (T1/2 α = 38.7 min; T1/2 β = 516.5 min). The biodistribution profile and scintigraphic images showed higher tumor uptake compared to contralateral muscle in all time-points investigated. Antitumor activity studies showed a substantial tumor growth inhibition ratio for NLC-DHA-DOX formulation. In addition, the formulation showed more favorable toxicity profiles when compared to equivalent doses of free administered drugs, being able to reduce heart and liver damage. CONCLUSIONS: Therefore, NLC-DHA-DOX formulation demonstrated feasibility in breast cancer treatment and diagnosis/monitoring, leading to a new possibility of a theranostic platform.
Authors: M E R O'Brien; N Wigler; M Inbar; R Rosso; E Grischke; A Santoro; R Catane; D G Kieback; P Tomczak; S P Ackland; F Orlandi; L Mellars; L Alland; C Tendler Journal: Ann Oncol Date: 2004-03 Impact factor: 32.976
Authors: Cristina Carvalho; Renato X Santos; Susana Cardoso; Sónia Correia; Paulo J Oliveira; Maria S Santos; Paula I Moreira Journal: Curr Med Chem Date: 2009-09-01 Impact factor: 4.530
Authors: Gustavo Henrique Rodrigues da Silva; Ludmilla David de Moura; Fabíola Vieira de Carvalho; Gabriela Geronimo; Talita Cesarim Mendonça; Fernando Freitas de Lima; Eneida de Paula Journal: Molecules Date: 2021-11-17 Impact factor: 4.411
Authors: Janaina de Alcantara Lemos; Anna Eliza M F M Oliveira; Raquel Silva Araujo; Danyelle M Townsend; Lucas Antonio Miranda Ferreira; Andre Luis Branco de Barros Journal: Biomed Pharmacother Date: 2021-09-07 Impact factor: 6.529