Folate-grafted glycyl-glycine-melphalan conjugate self-assembled amphilphilc nanomicelles augmented drug delivery, cytotoxicity and cellular uptake in human ovarian cancer cells
OBJECTIVES: Folic acid was coupled to melphalan using glycyl-glycine (FA-Gly-Gly-Melphalan) to synthesise self-assembled nanomicelles for targeting ovarian cancer cells, SKOV3.
METHODS AND RESULTS: FA-Gly-Gly-Melphalan self-assembled nanomicelles were prepared with critical micellar concentration (CMC) of 12-μg/ml. The mean particle size of FA-Gly-Gly-Melphalan self-assembled nanomicelles was measured to be 95.9 ± 3.4-nm significantly (p < 0.05) higher than 73.8 ± 6.3-nm of Gly-Gly-Melphalan self-assembled nanomicelles. Subsequently, zeta-potential of FA-Gly-Gly-Melphalan self-assembled nanomicelles was estimated to be -28.0 ± 1.5-mV significantly (p < 0.05) lower than -36.6 ± 2.7-mV of Gly-Gly-Melphalan self-assembled nanomicelles. The IC50 of FA-Gly-Gly-Melphalan self-assembled nanomicelles was estimated to be 4.1-μg/ml significantly (p < 0.001) lower than 14.2-μg/ml of Gly-Gly-Melphalan self-assembled nanomicelles and >18-μg/ml of melphalan. FA-Gly-Gly-Melphalan self-assembled nanomicelles preferentially accumulated in cytoplasm of SKOV3 cells nearby nucleus via receptor mediated endocytosis pathway after 24-h of incubation period, whilst Gly-Gly-Melphalan self-assembled nanomicelles were not incorporated sufficiently.
CONCLUSION: FA-Gly-Gly-Melphalan self-assembled nanomicelles warrant in depth in vivo study for their safety, efficacy, and potency in clinical settings.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:39 |
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| Enthalten in: |
Journal of microencapsulation - 39(2022), 3 vom: 15. Mai, Seite 197-209 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Duan, Jie [VerfasserIn] |
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| Links: |
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| Themen: |
10525P22U0 |
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| Anmerkungen: |
Date Completed 06.07.2022 Date Revised 06.07.2022 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1080/02652048.2020.1714764 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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NLM305357328 |
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| 245 | 1 | 0 | |a Folate-grafted glycyl-glycine-melphalan conjugate self-assembled amphilphilc nanomicelles augmented drug delivery, cytotoxicity and cellular uptake in human ovarian cancer cells |
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| 500 | |a Date Revised 06.07.2022 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a OBJECTIVES: Folic acid was coupled to melphalan using glycyl-glycine (FA-Gly-Gly-Melphalan) to synthesise self-assembled nanomicelles for targeting ovarian cancer cells, SKOV3 | ||
| 520 | |a METHODS AND RESULTS: FA-Gly-Gly-Melphalan self-assembled nanomicelles were prepared with critical micellar concentration (CMC) of 12-μg/ml. The mean particle size of FA-Gly-Gly-Melphalan self-assembled nanomicelles was measured to be 95.9 ± 3.4-nm significantly (p < 0.05) higher than 73.8 ± 6.3-nm of Gly-Gly-Melphalan self-assembled nanomicelles. Subsequently, zeta-potential of FA-Gly-Gly-Melphalan self-assembled nanomicelles was estimated to be -28.0 ± 1.5-mV significantly (p < 0.05) lower than -36.6 ± 2.7-mV of Gly-Gly-Melphalan self-assembled nanomicelles. The IC50 of FA-Gly-Gly-Melphalan self-assembled nanomicelles was estimated to be 4.1-μg/ml significantly (p < 0.001) lower than 14.2-μg/ml of Gly-Gly-Melphalan self-assembled nanomicelles and >18-μg/ml of melphalan. FA-Gly-Gly-Melphalan self-assembled nanomicelles preferentially accumulated in cytoplasm of SKOV3 cells nearby nucleus via receptor mediated endocytosis pathway after 24-h of incubation period, whilst Gly-Gly-Melphalan self-assembled nanomicelles were not incorporated sufficiently | ||
| 520 | |a CONCLUSION: FA-Gly-Gly-Melphalan self-assembled nanomicelles warrant in depth in vivo study for their safety, efficacy, and potency in clinical settings | ||
| 650 | 4 | |a Journal Article | |
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| 700 | 1 | |a Xiao, Xiao |e verfasserin |4 aut | |
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