Self-Assembling Hybrid Linear-Dendritic Block Copolymers: The Design of Nano-Carriers for Lipophilic Antitumoral Drugs
Two series of amphiphilic block copolymers with a hybrid linear-dendritic structure are presented. The compounds consisted of a hydrophilic poly (ethylene glycol) (PEG) block and a 2,2′-bis(hydroxymethyl)propionic acid (bis-MPA) dendron functionalized with stearic acid chains that impart a...
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| Format: | Article |
| Language: | English |
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MDPI AG
2019-01-01
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| Series: | Nanomaterials |
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| Online Access: | https://www.mdpi.com/2079-4991/9/2/161 |
| _version_ | 1818999794701434880 |
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| author | Elisabetta Fedeli Alexandre Lancelot Juan Manuel Dominguez José Luis Serrano Pilar Calvo Teresa Sierra |
| author_facet | Elisabetta Fedeli Alexandre Lancelot Juan Manuel Dominguez José Luis Serrano Pilar Calvo Teresa Sierra |
| author_sort | Elisabetta Fedeli |
| collection | DOAJ |
| description | Two series of amphiphilic block copolymers with a hybrid linear-dendritic structure are presented. The compounds consisted of a hydrophilic poly (ethylene glycol) (PEG) block and a 2,2′-bis(hydroxymethyl)propionic acid (bis-MPA) dendron functionalized with stearic acid chains that impart a hydrophobic nature to the block. Different self-assembled nanostructures with a hydrophobic interior and a hydrophilic external part were obtained depending on the length of the PEG chain (<i>M</i><sub>n</sub> = 2000 and <i>M</i><sub>n</sub> = 5000) and the generation of the bis-MPA dendron. The materials were characterized by transmission electron microscopy (TEM). The shapes of the aggregates ranged from spherical or cylindrical micelles to flexible bilayers. The hydrophobic core enabled these nanostructures to encapsulate the water-insoluble drug plitidepsin. The efficacy of these new plitidepsin-containing carriers was evaluated in four cancer cell-lines and they showed similar anticancer activity to the current standard drug formulation. |
| first_indexed | 2024-12-20T22:23:05Z |
| format | Article |
| id | doaj.art-e7f1ec9191dd4a228d4654e6ea481e60 |
| institution | Directory Open Access Journal |
| issn | 2079-4991 |
| language | English |
| last_indexed | 2024-12-20T22:23:05Z |
| publishDate | 2019-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Nanomaterials |
| spelling | doaj.art-e7f1ec9191dd4a228d4654e6ea481e602022-12-21T19:24:53ZengMDPI AGNanomaterials2079-49912019-01-019216110.3390/nano9020161nano9020161Self-Assembling Hybrid Linear-Dendritic Block Copolymers: The Design of Nano-Carriers for Lipophilic Antitumoral DrugsElisabetta Fedeli0Alexandre Lancelot1Juan Manuel Dominguez2José Luis Serrano3Pilar Calvo4Teresa Sierra5Departamento de Química Orgánica, Instituto de Nanociencia de Aragón (INA), Instituto de Ciencia de Materiales de Aragón (ICMA), Edificio I+D, Universidad de Zaragoza, 50018 Zaragoza, SpainDepartamento de Química Orgánica, Instituto de Nanociencia de Aragón (INA), Instituto de Ciencia de Materiales de Aragón (ICMA), Edificio I+D, Universidad de Zaragoza, 50018 Zaragoza, SpainPharmaMar S.A., 28770 Colmenar Viejo, Madrid, SpainDepartamento de Química Orgánica, Instituto de Nanociencia de Aragón (INA), Instituto de Ciencia de Materiales de Aragón (ICMA), Edificio I+D, Universidad de Zaragoza, 50018 Zaragoza, SpainPharmaMar S.A., 28770 Colmenar Viejo, Madrid, SpainDepartamento de Química Orgánica, Instituto de Ciencia de Materiales de Aragón (ICMA), Facultad de Ciencias, CSIC, Universidad de Zaragoza, 50009 Zaragoza, SpainTwo series of amphiphilic block copolymers with a hybrid linear-dendritic structure are presented. The compounds consisted of a hydrophilic poly (ethylene glycol) (PEG) block and a 2,2′-bis(hydroxymethyl)propionic acid (bis-MPA) dendron functionalized with stearic acid chains that impart a hydrophobic nature to the block. Different self-assembled nanostructures with a hydrophobic interior and a hydrophilic external part were obtained depending on the length of the PEG chain (<i>M</i><sub>n</sub> = 2000 and <i>M</i><sub>n</sub> = 5000) and the generation of the bis-MPA dendron. The materials were characterized by transmission electron microscopy (TEM). The shapes of the aggregates ranged from spherical or cylindrical micelles to flexible bilayers. The hydrophobic core enabled these nanostructures to encapsulate the water-insoluble drug plitidepsin. The efficacy of these new plitidepsin-containing carriers was evaluated in four cancer cell-lines and they showed similar anticancer activity to the current standard drug formulation.https://www.mdpi.com/2079-4991/9/2/161dendrimersmicellar aggregatesdrug deliveryanticancer |
| spellingShingle | Elisabetta Fedeli Alexandre Lancelot Juan Manuel Dominguez José Luis Serrano Pilar Calvo Teresa Sierra Self-Assembling Hybrid Linear-Dendritic Block Copolymers: The Design of Nano-Carriers for Lipophilic Antitumoral Drugs Nanomaterials dendrimers micellar aggregates drug delivery anticancer |
| title | Self-Assembling Hybrid Linear-Dendritic Block Copolymers: The Design of Nano-Carriers for Lipophilic Antitumoral Drugs |
| title_full | Self-Assembling Hybrid Linear-Dendritic Block Copolymers: The Design of Nano-Carriers for Lipophilic Antitumoral Drugs |
| title_fullStr | Self-Assembling Hybrid Linear-Dendritic Block Copolymers: The Design of Nano-Carriers for Lipophilic Antitumoral Drugs |
| title_full_unstemmed | Self-Assembling Hybrid Linear-Dendritic Block Copolymers: The Design of Nano-Carriers for Lipophilic Antitumoral Drugs |
| title_short | Self-Assembling Hybrid Linear-Dendritic Block Copolymers: The Design of Nano-Carriers for Lipophilic Antitumoral Drugs |
| title_sort | self assembling hybrid linear dendritic block copolymers the design of nano carriers for lipophilic antitumoral drugs |
| topic | dendrimers micellar aggregates drug delivery anticancer |
| url | https://www.mdpi.com/2079-4991/9/2/161 |
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