Journal
MOLECULAR IMAGING AND BIOLOGY
Volume 20, Issue 3, Pages 437-447Publisher
SPRINGER
DOI: 10.1007/s11307-017-1133-3
Keywords
Docosahexaenoic acid; Doxorubicin; Nanostructured lipid carrier; Tc-99m; Theranostic
Funding
- Fundacao de Amparo a Pesquisa do Estado de Minas Gerais (FAPEMIG-Brazil)
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq-Brazil)
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES-Brazil)
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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. 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. NCL was successfully radiolabeled with Tc-99m. Blood clearance showed a relatively long half-life, with blood levels decaying in a biphasic manner (T-1/2 alpha = 38.7 min; T-1/2 beta = 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. Therefore, NLC-DHA-DOX formulation demonstrated feasibility in breast cancer treatment and diagnosis/monitoring, leading to a new possibility of a theranostic platform.
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