Branched Poly(<i>ε</i>-caprolactone)-Based Copolyesters of Different Architectures and Their Use in the Preparation of Anticancer Drug-Loaded Nanoparticles
Limitations associated with the use of linear biodegradable polyesters in the preparation of anticancer nano-based drug delivery systems (nanoDDS) have turned scientific attention to the utilization of branched-chain (co-)polymers. In this context, the present study evaluates the use of novel branch...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-12-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/23/23/15393 |
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| author | Evi Christodoulou Maria Notopoulou Eirini Nakiou Margaritis Kostoglou Panagiotis Barmpalexis Dimitrios N. Bikiaris |
| author_facet | Evi Christodoulou Maria Notopoulou Eirini Nakiou Margaritis Kostoglou Panagiotis Barmpalexis Dimitrios N. Bikiaris |
| author_sort | Evi Christodoulou |
| collection | DOAJ |
| description | Limitations associated with the use of linear biodegradable polyesters in the preparation of anticancer nano-based drug delivery systems (nanoDDS) have turned scientific attention to the utilization of branched-chain (co-)polymers. In this context, the present study evaluates the use of novel branched poly(ε-caprolactone) (PCL)-based copolymers of different architectures for the preparation of anticancer nanoparticle (NP)-based formulations, using paclitaxel (PTX) as a model drug. Specifically, three PCL-polyol branched polyesters, namely, a three-arm copolymer based on glycerol (PCL-GLY), a four-arm copolymer based on pentaerythritol (PCL-PE), and a five-arm copolymer based on xylitol (PCL-XYL), were synthesized via ring-opening polymerization and characterized by proton nuclear magnetic resonance (<sup>1</sup>H-NMR), gel permeation chromatography (GPC), intrinsic viscosity, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier-transform infrared (FT-IR) spectroscopy and cytotoxicity. Then, PTX-loaded NPs were prepared by an oil-in-water emulsion. The size of the obtained NPs varied from 200 to 300 nm, while the drug was dispersed in crystalline form in all formulations. High encapsulation efficiency and high yields were obtained in all cases, while FTIR analysis showed no molecular drug polymer. Finally, in vitro drug release studies showed that the studied nanocarriers significantly enhanced the dissolution rate and extent of the drug. |
| first_indexed | 2024-03-09T17:44:56Z |
| format | Article |
| id | doaj.art-d72e47428c414b25974bc154fc60c84f |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-09T17:44:56Z |
| publishDate | 2022-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-d72e47428c414b25974bc154fc60c84f2023-11-24T11:18:18ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672022-12-0123231539310.3390/ijms232315393Branched Poly(<i>ε</i>-caprolactone)-Based Copolyesters of Different Architectures and Their Use in the Preparation of Anticancer Drug-Loaded NanoparticlesEvi Christodoulou0Maria Notopoulou1Eirini Nakiou2Margaritis Kostoglou3Panagiotis Barmpalexis4Dimitrios N. Bikiaris5Laboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, GreeceLaboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, GreeceLaboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, GreeceLaboratory of General and Inorganic Chemical Technology, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, GreeceDepartment of Pharmaceutical Technology, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, GreeceLaboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, GreeceLimitations associated with the use of linear biodegradable polyesters in the preparation of anticancer nano-based drug delivery systems (nanoDDS) have turned scientific attention to the utilization of branched-chain (co-)polymers. In this context, the present study evaluates the use of novel branched poly(ε-caprolactone) (PCL)-based copolymers of different architectures for the preparation of anticancer nanoparticle (NP)-based formulations, using paclitaxel (PTX) as a model drug. Specifically, three PCL-polyol branched polyesters, namely, a three-arm copolymer based on glycerol (PCL-GLY), a four-arm copolymer based on pentaerythritol (PCL-PE), and a five-arm copolymer based on xylitol (PCL-XYL), were synthesized via ring-opening polymerization and characterized by proton nuclear magnetic resonance (<sup>1</sup>H-NMR), gel permeation chromatography (GPC), intrinsic viscosity, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier-transform infrared (FT-IR) spectroscopy and cytotoxicity. Then, PTX-loaded NPs were prepared by an oil-in-water emulsion. The size of the obtained NPs varied from 200 to 300 nm, while the drug was dispersed in crystalline form in all formulations. High encapsulation efficiency and high yields were obtained in all cases, while FTIR analysis showed no molecular drug polymer. Finally, in vitro drug release studies showed that the studied nanocarriers significantly enhanced the dissolution rate and extent of the drug.https://www.mdpi.com/1422-0067/23/23/15393poly(ε-caprolactone)ring-opening polymerizationbranched copolymersnanoparticlesanticancerpaclitaxel |
| spellingShingle | Evi Christodoulou Maria Notopoulou Eirini Nakiou Margaritis Kostoglou Panagiotis Barmpalexis Dimitrios N. Bikiaris Branched Poly(<i>ε</i>-caprolactone)-Based Copolyesters of Different Architectures and Their Use in the Preparation of Anticancer Drug-Loaded Nanoparticles International Journal of Molecular Sciences poly(ε-caprolactone) ring-opening polymerization branched copolymers nanoparticles anticancer paclitaxel |
| title | Branched Poly(<i>ε</i>-caprolactone)-Based Copolyesters of Different Architectures and Their Use in the Preparation of Anticancer Drug-Loaded Nanoparticles |
| title_full | Branched Poly(<i>ε</i>-caprolactone)-Based Copolyesters of Different Architectures and Their Use in the Preparation of Anticancer Drug-Loaded Nanoparticles |
| title_fullStr | Branched Poly(<i>ε</i>-caprolactone)-Based Copolyesters of Different Architectures and Their Use in the Preparation of Anticancer Drug-Loaded Nanoparticles |
| title_full_unstemmed | Branched Poly(<i>ε</i>-caprolactone)-Based Copolyesters of Different Architectures and Their Use in the Preparation of Anticancer Drug-Loaded Nanoparticles |
| title_short | Branched Poly(<i>ε</i>-caprolactone)-Based Copolyesters of Different Architectures and Their Use in the Preparation of Anticancer Drug-Loaded Nanoparticles |
| title_sort | branched poly i ε i caprolactone based copolyesters of different architectures and their use in the preparation of anticancer drug loaded nanoparticles |
| topic | poly(ε-caprolactone) ring-opening polymerization branched copolymers nanoparticles anticancer paclitaxel |
| url | https://www.mdpi.com/1422-0067/23/23/15393 |
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