Formulation, Characterization and Evaluation against SH-SY5Y Cells of New Tacrine and Tacrine-MAP Loaded with Lipid Nanoparticles
Tacrine (TAC) was the first FDA approved drug for the treatment of Alzheimer’s disease, resulting in increased memory and enhanced cognitive symptoms in patients. However, long-term therapy presents poor patient compliance associated with undesired side effects such as nausea, vomiting and hepatoxic...
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doaj-44b7323b6be1418fb6ad992a7cc1659f2020-11-25T03:41:47ZengMDPI AGNanomaterials2079-49912020-10-01102089208910.3390/nano10102089Formulation, Characterization and Evaluation against SH-SY5Y Cells of New Tacrine and Tacrine-MAP Loaded with Lipid NanoparticlesSara Silva0Joana Marto1Lídia Gonçalves2António J. Almeida3Nuno Vale4OncoPharma Research Group, Center for Health Technology and Services Research (CINTESIS), Rua Dr. Plácido da Costa, 4200-450 Porto, PortugalResearch Institute for Medicines (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, Avenida Prof. Gama Pinto, 1649-003 Lisboa, PortugalResearch Institute for Medicines (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, Avenida Prof. Gama Pinto, 1649-003 Lisboa, PortugalResearch Institute for Medicines (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, Avenida Prof. Gama Pinto, 1649-003 Lisboa, PortugalOncoPharma Research Group, Center for Health Technology and Services Research (CINTESIS), Rua Dr. Plácido da Costa, 4200-450 Porto, PortugalTacrine (TAC) was the first FDA approved drug for the treatment of Alzheimer’s disease, resulting in increased memory and enhanced cognitive symptoms in patients. However, long-term therapy presents poor patient compliance associated with undesired side effects such as nausea, vomiting and hepatoxicity. To improve its therapeutic efficacy and decrease toxicity, the use of nanoparticles could be applied as a possible solution to delivery TAC. In this context, a project has been designed to develop a new nanostructured lipid carrier (NLC) as a delivery system for TAC and conjugate TAC and model amphipathic peptide (MAP) to decrease TAC limitations. Different formulations loaded with TAC and TAC + MAP were prepared using a combination of Compritol 888 ATO as the solid lipid and Transcutol HP as the liquid lipid component. Physical characterization was evaluated in terms of particle size, surface charge, encapsulation efficiency and in vitro drug release studies. Particle size distributions within the nanometer range were obtained with encapsulation efficiencies of 72.4% for the TAC and 85.6% for the TAC + MAP conjugate. Furthermore, cytotoxicity of all NLC formulations was determined against neuroblastoma cell line SH-SY5Y. The optimized TAC delivery system revealed low toxicity suggesting this could be a potential carrier system to deliver TAC. However, TAC + MAP conjugated even encapsulated in the NLC system demonstrated toxicity against the SH-SY5Y cell line.https://www.mdpi.com/2079-4991/10/10/2089tacrinenanoparticlesSH-SY5YMAPAlzheimer’s diseasedrug delivery |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Sara Silva Joana Marto Lídia Gonçalves António J. Almeida Nuno Vale |
spellingShingle |
Sara Silva Joana Marto Lídia Gonçalves António J. Almeida Nuno Vale Formulation, Characterization and Evaluation against SH-SY5Y Cells of New Tacrine and Tacrine-MAP Loaded with Lipid Nanoparticles Nanomaterials tacrine nanoparticles SH-SY5Y MAP Alzheimer’s disease drug delivery |
author_facet |
Sara Silva Joana Marto Lídia Gonçalves António J. Almeida Nuno Vale |
author_sort |
Sara Silva |
title |
Formulation, Characterization and Evaluation against SH-SY5Y Cells of New Tacrine and Tacrine-MAP Loaded with Lipid Nanoparticles |
title_short |
Formulation, Characterization and Evaluation against SH-SY5Y Cells of New Tacrine and Tacrine-MAP Loaded with Lipid Nanoparticles |
title_full |
Formulation, Characterization and Evaluation against SH-SY5Y Cells of New Tacrine and Tacrine-MAP Loaded with Lipid Nanoparticles |
title_fullStr |
Formulation, Characterization and Evaluation against SH-SY5Y Cells of New Tacrine and Tacrine-MAP Loaded with Lipid Nanoparticles |
title_full_unstemmed |
Formulation, Characterization and Evaluation against SH-SY5Y Cells of New Tacrine and Tacrine-MAP Loaded with Lipid Nanoparticles |
title_sort |
formulation, characterization and evaluation against sh-sy5y cells of new tacrine and tacrine-map loaded with lipid nanoparticles |
publisher |
MDPI AG |
series |
Nanomaterials |
issn |
2079-4991 |
publishDate |
2020-10-01 |
description |
Tacrine (TAC) was the first FDA approved drug for the treatment of Alzheimer’s disease, resulting in increased memory and enhanced cognitive symptoms in patients. However, long-term therapy presents poor patient compliance associated with undesired side effects such as nausea, vomiting and hepatoxicity. To improve its therapeutic efficacy and decrease toxicity, the use of nanoparticles could be applied as a possible solution to delivery TAC. In this context, a project has been designed to develop a new nanostructured lipid carrier (NLC) as a delivery system for TAC and conjugate TAC and model amphipathic peptide (MAP) to decrease TAC limitations. Different formulations loaded with TAC and TAC + MAP were prepared using a combination of Compritol 888 ATO as the solid lipid and Transcutol HP as the liquid lipid component. Physical characterization was evaluated in terms of particle size, surface charge, encapsulation efficiency and in vitro drug release studies. Particle size distributions within the nanometer range were obtained with encapsulation efficiencies of 72.4% for the TAC and 85.6% for the TAC + MAP conjugate. Furthermore, cytotoxicity of all NLC formulations was determined against neuroblastoma cell line SH-SY5Y. The optimized TAC delivery system revealed low toxicity suggesting this could be a potential carrier system to deliver TAC. However, TAC + MAP conjugated even encapsulated in the NLC system demonstrated toxicity against the SH-SY5Y cell line. |
topic |
tacrine nanoparticles SH-SY5Y MAP Alzheimer’s disease drug delivery |
url |
https://www.mdpi.com/2079-4991/10/10/2089 |
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