Talazoparib Loaded Solid Lipid Nanoparticles : Preparation, Characterization and Evaluation of the Therapeutic Efficacy In vitro
Copyright© Bentham Science Publishers; For any queries, please email at epubbenthamscience.net..
OBJECTIVE: In the present work, we report for the first time the therapeutic potential of talazoparib (BMN 673)-SLNs for the treatment of BRCA1 deficient Triple Negative Breast Cancer (TNBC). BMN 673-SLNs were produced by hot-homogenization technique and then characterized.
METHODS: The cytotoxic and apoptotic effects of BMN 673-SLNs compared with BMN 673 were determined on HCC1937BRCA1-/-, HCC1937-R resistant TNBC and MCF-10A control cell lines. BMN 673- SLNs were found to have reduced particle size (219.5 ± 1.45 nm) and thus more stable (-28.4 ± 2.52 mV) than BMN 673 (1652 ± 2.46 nm and -18.6 ± 0.45 mV) at 4°C.
RESULTS: In vitro cell line studies demonstrated that BMN 673-SLNs showed significant cytotoxic effects on HCC1937 (29.8%) and HCC1937-R cells (35.7%) at 10 nM for 12 days compared with BMN 673 (HCC1937 cells: 34.0% and HCC1937-R cells: 93.8% at 10 nM for 12 days) (p<0.05). Additionally, BMN 673-SLNs (40.1%) reduced the toxicity of BMN 673 (53.1%) on MCF-10A control cells thanks to unique physical properties.
CONCLUSION: The apoptotic rates in the 10 nM BMN 673-SLNs treatment (88.78% and 85.56%) for 12 days were significantly higher than those in 10 nM BMN 673 (82.6% and 25.86%) for 12 days in HCC1937 and HCC1937-R cells, respectively (p<0.01). Furthermore, these effects were consistent with the findings of colony formation, wound healing and calcein accumulation analysis. In conclusion, the therapeutic potential of BMN 673-SLNs provides a promising chemotherapeutic strategy for the treatment of drugresistant TNBC.
Medienart: |
E-Artikel |
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Erscheinungsjahr: |
2019 |
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Erschienen: |
2019 |
Enthalten in: |
Zur Gesamtaufnahme - volume:16 |
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Enthalten in: |
Current drug delivery - 16(2019), 6 vom: 31., Seite 511-529 |
Sprache: |
Englisch |
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Beteiligte Personen: |
Eskiler, Gamze Guney [VerfasserIn] |
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Links: |
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Anmerkungen: |
Date Completed 23.03.2020 Date Revised 23.03.2020 published: Print Citation Status MEDLINE |
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doi: |
10.2174/1567201816666190515105532 |
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funding: |
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Förderinstitution / Projekttitel: |
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PPN (Katalog-ID): |
NLM297317245 |
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520 | |a OBJECTIVE: In the present work, we report for the first time the therapeutic potential of talazoparib (BMN 673)-SLNs for the treatment of BRCA1 deficient Triple Negative Breast Cancer (TNBC). BMN 673-SLNs were produced by hot-homogenization technique and then characterized | ||
520 | |a METHODS: The cytotoxic and apoptotic effects of BMN 673-SLNs compared with BMN 673 were determined on HCC1937BRCA1-/-, HCC1937-R resistant TNBC and MCF-10A control cell lines. BMN 673- SLNs were found to have reduced particle size (219.5 ± 1.45 nm) and thus more stable (-28.4 ± 2.52 mV) than BMN 673 (1652 ± 2.46 nm and -18.6 ± 0.45 mV) at 4°C | ||
520 | |a RESULTS: In vitro cell line studies demonstrated that BMN 673-SLNs showed significant cytotoxic effects on HCC1937 (29.8%) and HCC1937-R cells (35.7%) at 10 nM for 12 days compared with BMN 673 (HCC1937 cells: 34.0% and HCC1937-R cells: 93.8% at 10 nM for 12 days) (p<0.05). Additionally, BMN 673-SLNs (40.1%) reduced the toxicity of BMN 673 (53.1%) on MCF-10A control cells thanks to unique physical properties | ||
520 | |a CONCLUSION: The apoptotic rates in the 10 nM BMN 673-SLNs treatment (88.78% and 85.56%) for 12 days were significantly higher than those in 10 nM BMN 673 (82.6% and 25.86%) for 12 days in HCC1937 and HCC1937-R cells, respectively (p<0.01). Furthermore, these effects were consistent with the findings of colony formation, wound healing and calcein accumulation analysis. In conclusion, the therapeutic potential of BMN 673-SLNs provides a promising chemotherapeutic strategy for the treatment of drugresistant TNBC | ||
650 | 4 | |a Journal Article | |
650 | 4 | |a Apoptosis | |
650 | 4 | |a PARP inhibitors | |
650 | 4 | |a Solid Lipid Nanoparticles(SLNs) | |
650 | 4 | |a Talazoparib (BMN 673) | |
650 | 4 | |a Triple Negative Breast Cancer (TNBC) | |
650 | 4 | |a cytotoxic effects. | |
650 | 7 | |a Antineoplastic Agents |2 NLM | |
650 | 7 | |a BRCA1 Protein |2 NLM | |
650 | 7 | |a BRCA1 protein, human |2 NLM | |
650 | 7 | |a Lipids |2 NLM | |
650 | 7 | |a Phthalazines |2 NLM | |
650 | 7 | |a talazoparib |2 NLM | |
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700 | 1 | |a Tunca, Berrin |e verfasserin |4 aut | |
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