11 results on '"Izabela Kurowska"'
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2. Synergistic effect of folate-conjugated polymers and 5-fluorouracil in the treatment of colon cancer
- Author
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Gabriela Siemiaszko, Katarzyna Niemirowicz-Laskowska, Karolina H. Markiewicz, Iwona Misztalewska-Turkowicz, Ewelina Dudź, Sylwia Milewska, Paweł Misiak, Izabela Kurowska, Anna Sadowska, Halina Car, and Agnieszka Z. Wilczewska
- Subjects
Folic acid ,Colon cancer ,5-Fluorouracil ,Drug delivery system ,Targeted therapy ,RAFT/MADIX polymerization ,Neoplasms. Tumors. Oncology. Including cancer and carcinogens ,RC254-282 - Abstract
Abstract Background In recent years, targeted drug delivery strategies have received special attention from the scientific world due to advantages such as more effective therapy and reduction of side effects. The principle of operation is delayed excretion from the bloodstream of the drug delivery system compared to the drug itself, as well as facilitated penetration into diseased cells thanks to the use of ligands recognized by appropriate receptors. Particularly interesting drug carriers are amphiphilic copolymers that form nano-sized micelles with a drug, which can release the drug at a specific place in the body under the influence of appropriate stimuli. Results We describe the synthesis of the diblock polymer, poly(2-hydroxyethyl acrylate)-b-poly(N-vinylcaprolactam) using RAFT/MADIX (Reversible Addition-Fragmentation chain Transfer/MAcromolecular Design by Interchange of Xanthate) controlled polymerization affording polymers with good dispersity according to SEC (Size-Exclusion Chromatography). Some post-modifications of the polymer with folic acid were then performed as evidenced by NMR (Nuclear Magnetic Resonance), UV–Vis (UltraViolet–Visible) and FT-IR (Fourier-Transform Infrared) spectroscopy, and TGA (ThermoGravimetric Analysis). The formation of stable micellar systems from polymers with and without the drug, 5-fluorouracil, was confirmed by DLS (Dynamic Light Scattering) and zeta potential measurements, and TEM (Transmission Eelectron Microscopy) imaging. Finally, the cloud point of the polymers was investigated, which turned out to be close to the temperature of the human body. Most importantly, these micellar systems have been explored as a drug delivery system against colon cancer, showing increased cytotoxicity compared to the drug alone. This effect was achieved due to the easier cellular uptake by the interaction of folic acid and its receptors on the surface of cancer cells. Conclusions The presented results constitute a solid foundation for the implementation of a nano-sized drug delivery system containing folic acid for practical use in the treatment of drug-resistant cancer, as well as more effective therapy with fewer side effects. Graphical Abstract
- Published
- 2021
- Full Text
- View/download PDF
3. Multilayer Films Based on Chitosan/Pectin Polyelectrolyte Complexes as Novel Platforms for Buccal Administration of Clotrimazole
- Author
-
Joanna Potaś, Emilia Szymańska, Magdalena Wróblewska, Izabela Kurowska, Mateusz Maciejczyk, Anna Basa, Eliza Wolska, Agnieszka Zofia Wilczewska, and Katarzyna Winnicka
- Subjects
multilayer film ,polyelectrolyte complex ,chitosan ,pectin ,clotrimazole ,oral candidiasis ,Pharmacy and materia medica ,RS1-441 - Abstract
Buccal films are recognized as easily applicable, microbiologically stable drug dosage forms with good retentivity at the mucosa intended for the therapy of oromucosal conditions, especially infectious diseases. Multilayer films composed of layers of oppositely charged polymers separated by ionically interacting polymeric chains creating polyelectrolyte complexes represent very interesting and relatively poorly explored area. We aimed to develop the antifungal multilayer systems composed of cationic chitosan and anionic pectin as potential platforms for controlled delivery of clotrimazole. The systems were pharmaceutically characterized with regard to inter alia their release kinetics under different pH conditions, physicomechanical, or mucoadhesion properties with using an animal model of the buccal mucosa. The antifungal activity against selected Candida sp. and potential cytotoxicity with regard to human gingival fibroblasts were also evaluated. Interactions between polyions were characterized with Fourier transform infrared spectroscopy. Different clotrimazole distribution in the films layers highly affected their in vitro dissolution profile. The designed films were recognized as intelligent pH-responsive systems with strong antifungal effect and satisfactory safety profile. As addition of chitosan resulted in the improved antifungal behavior of the drug, the potential utilization of the films in resistant cases of oral candidiasis might be worth of further exploration.
- Published
- 2021
- Full Text
- View/download PDF
4. Versatile thiolactone-based conjugation strategies to polymer stabilizers for multifunctional upconverting nanoparticles aqueous dispersions
- Author
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Izabela Kurowska, Baptiste Amouroux, Marvin Langlais, Olivier Coutelier, Christophe Coudret, Mathias Destarac, Jean-Daniel Marty, Interactions moléculaires et réactivité chimique et photochimique (IMRCP), Institut de Chimie de Toulouse (ICT), Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Université de Toulouse (UT)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université de Toulouse (UT)-Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Institut Ecologie et Environnement (INEE), Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS)-Fédération de Recherche Fluides, Energie, Réacteurs, Matériaux et Transferts (FERMAT), Institut National des Sciences Appliquées - Toulouse (INSA Toulouse), Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Centre National de la Recherche Scientifique (CNRS)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université de Toulouse (UT)-Institut National des Sciences Appliquées - Toulouse (INSA Toulouse), Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Institut National des Sciences Appliquées (INSA)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS), IDeAS - Interfaces Dynamiques et Assemblages Stimulables (IDeAS), Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Institut National des Sciences Appliquées (INSA)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie de Toulouse (ICT), and P3R - Polymères de Précision par Procédés Radicalaires (P3R)
- Subjects
[CHIM]Chemical Sciences ,General Materials Science - Abstract
International audience; Well-defined phosphonic acid-terminated polymers were synthesized from amine-terminated polymer precursors and a phosphonated thiolactone and were used to prepare stable, water-dispersible multifunctional upconverting luminescent nanohybrids.
- Published
- 2022
5. Synergistic effect of folate-conjugated polymers and 5-fluorouracil in the treatment of colon cancer
- Author
-
Izabela Kurowska, Karolina H. Markiewicz, Iwona Misztalewska-Turkowicz, Agnieszka Z. Wilczewska, Anna Sadowska, Paweł Misiak, Gabriela Siemiaszko, Sylwia Milewska, Halina Car, Katarzyna Niemirowicz-Laskowska, and Ewelina Dudź
- Subjects
Drug ,Folic acid ,Chemistry ,media_common.quotation_subject ,5-Fluorouracil ,Dispersity ,Drug delivery system ,Biomedical Engineering ,Pharmaceutical Science ,Neoplasms. Tumors. Oncology. Including cancer and carcinogens ,Conjugated system ,Combinatorial chemistry ,Micelle ,Colon cancer ,Targeted therapy ,RAFT/MADIX polymerization ,Oncology ,Targeted drug delivery ,Dynamic light scattering ,Drug delivery ,Physical and Theoretical Chemistry ,Drug carrier ,RC254-282 ,media_common - Abstract
Background In recent years, targeted drug delivery strategies have received special attention from the scientific world due to advantages such as more effective therapy and reduction of side effects. The principle of operation is delayed excretion from the bloodstream of the drug delivery system compared to the drug itself, as well as facilitated penetration into diseased cells thanks to the use of ligands recognized by appropriate receptors. Particularly interesting drug carriers are amphiphilic copolymers that form nano-sized micelles with a drug, which can release the drug at a specific place in the body under the influence of appropriate stimuli. Results We describe the synthesis of the diblock polymer, poly(2-hydroxyethyl acrylate)-b-poly(N-vinylcaprolactam) using RAFT/MADIX (Reversible Addition-Fragmentation chain Transfer/MAcromolecular Design by Interchange of Xanthate) controlled polymerization affording polymers with good dispersity according to SEC (Size-Exclusion Chromatography). Some post-modifications of the polymer with folic acid were then performed as evidenced by NMR (Nuclear Magnetic Resonance), UV–Vis (UltraViolet–Visible) and FT-IR (Fourier-Transform Infrared) spectroscopy, and TGA (ThermoGravimetric Analysis). The formation of stable micellar systems from polymers with and without the drug, 5-fluorouracil, was confirmed by DLS (Dynamic Light Scattering) and zeta potential measurements, and TEM (Transmission Eelectron Microscopy) imaging. Finally, the cloud point of the polymers was investigated, which turned out to be close to the temperature of the human body. Most importantly, these micellar systems have been explored as a drug delivery system against colon cancer, showing increased cytotoxicity compared to the drug alone. This effect was achieved due to the easier cellular uptake by the interaction of folic acid and its receptors on the surface of cancer cells. Conclusions The presented results constitute a solid foundation for the implementation of a nano-sized drug delivery system containing folic acid for practical use in the treatment of drug-resistant cancer, as well as more effective therapy with fewer side effects. Graphical Abstract
- Published
- 2021
6. Tailor-made poly(vinylamine) via purple LED-activated RAFT polymerization of N-vinylformamide
- Author
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Izabela Kurowska, Alexis Dupre–Demorsy, Stéphane Balayssac, Marie Hennetier, Audrey Ric, Valérie Bourdon, Tsuyoshi Ando, Hiroharu Ajiro, Olivier Coutelier, Mathias Destarac, Interactions moléculaires et réactivité chimique et photochimique (IMRCP), Institut de Chimie de Toulouse (ICT), Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Université de Toulouse (UT)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université de Toulouse (UT)-Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Institut Ecologie et Environnement (INEE), Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS)-Fédération de Recherche Fluides, Energie, Réacteurs, Matériaux et Transferts (FERMAT), Institut National des Sciences Appliquées - Toulouse (INSA Toulouse), Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Centre National de la Recherche Scientifique (CNRS)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université de Toulouse (UT)-Institut National des Sciences Appliquées - Toulouse (INSA Toulouse), Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Institut National des Sciences Appliquées (INSA)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS), P3R - Polymères de Précision par Procédés Radicalaires (P3R), Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Institut National des Sciences Appliquées (INSA)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie de Toulouse (ICT), BIBAC - Chimie analytique et interactions biomolécules - matière molle biomimétique (BIBAC), Institut National Polytechnique (Toulouse) (Toulouse INP), Université de Toulouse (UT), and Université Toulouse III - Paul Sabatier (UT3)
- Subjects
Polymers and Plastics ,Organic Chemistry ,Materials Chemistry ,[CHIM]Chemical Sciences - Abstract
Photo-iniferter reversible addition-fragmentation chain transfer (PI-RAFT) of N-vinylformamide (NVF) was demonstrated by using purple light. PNVFs with predetermined molar masses and narrow molar mass distributions were obtained. High RAFT chain-end fidelity was confirmed by MALDI-TOF and ESI-MS, and chain extension experiment. To demonstrate the potential of this approach, an original PVP-b-PNVF diblock copolymer was synthesized and characterized by aqueous SEC, A4F, and
- Published
- 2022
7. RAFT polymerisation of N -vinylformamide and the corresponding double hydrophilic block copolymers
- Author
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Alexis Dupre--Demorsy, Izabela Kurowska, Stéphane Balayssac, Marie Hennetier, Audrey Ric, Valérie Bourdon, Tsuyoshi Ando, Hiroharu Ajiro, Olivier Coutelier, Mathias Destarac, Interactions moléculaires et réactivité chimique et photochimique (IMRCP), Institut de Chimie de Toulouse (ICT), Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Université de Toulouse (UT)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université de Toulouse (UT)-Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Institut Ecologie et Environnement (INEE), Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS)-Fédération de Recherche Fluides, Energie, Réacteurs, Matériaux et Transferts (FERMAT), Institut National des Sciences Appliquées - Toulouse (INSA Toulouse), Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Centre National de la Recherche Scientifique (CNRS)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université de Toulouse (UT)-Institut National des Sciences Appliquées - Toulouse (INSA Toulouse), Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Institut National des Sciences Appliquées (INSA)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS), P3R - Polymères de Précision par Procédés Radicalaires (P3R), Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Institut National des Sciences Appliquées (INSA)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie de Toulouse (ICT), BIBAC - Chimie analytique et interactions biomolécules - matière molle biomimétique (BIBAC), Ecole d'Ingénieurs de Purpan (INP - PURPAN), Institut National Polytechnique (Toulouse) (Toulouse INP), Université de Toulouse (UT)-Université de Toulouse (UT), Université de Toulouse (UT), Service Commun de Spectrométrie de Masse (Toulouse, France), and Université Toulouse III - Paul Sabatier (UT3)
- Subjects
Polymers and Plastics ,Organic Chemistry ,[CHIM]Chemical Sciences ,Bioengineering ,Biochemistry - Abstract
Polyvinylamine-based double hydrophilic block copolymers are synthesised from RAFT polymerisation of N-vinylformamide.
- Published
- 2022
8. Evaluation of Cytotoxic Effect of Cholesterol End-Capped Poly(N-Isopropylacrylamide)s on Selected Normal and Neoplastic Cells
- Author
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Agnieszka Z. Wilczewska, Halina Car, Izabela Kurowska, Paweł Misiak, Karolina H. Markiewicz, Katarzyna Niemirowicz-Laskowska, Przemyslaw Wielgat, Iwona Misztalewska-Turkowicz, Gabriela Siemiaszko, and Mathias Destarac
- Subjects
Organic Chemistry ,Biophysics ,Pharmaceutical Science ,Bioengineering ,Chain transfer ,02 engineering and technology ,General Medicine ,Raft ,010402 general chemistry ,021001 nanoscience & nanotechnology ,01 natural sciences ,Micelle ,0104 chemical sciences ,Biomaterials ,chemistry.chemical_compound ,chemistry ,Targeted drug delivery ,Drug Discovery ,Drug delivery ,Poly(N-isopropylacrylamide) ,Moiety ,0210 nano-technology ,Drug carrier - Abstract
Purpose Efficient intracellular delivery of a therapeutic compound is an important feature of smart drug delivery systems (SDDS). Modification of a carrier structure with a cell-penetrating ligand, ie, cholesterol moiety, is a strategy to improve cellular uptake. Cholesterol end-capped poly(N-isopropylacrylamide)s offer a promising foundation for the design of efficient thermoresponsive drug delivery systems. Methods A series of cholesterol end-capped poly(N-isopropylacrylamide)s (PNIPAAm) with number-average molar masses ranging from 3200 to 11000 g·mol-1 were synthesized by reversible addition-fragmentation chain transfer (RAFT) polymerization from original xanthate-functionalized cholesterol and self-assembled into micelles. The physicochemical characteristics and cytotoxicity of cholesterol end-capped poly(N-isopropylacrylamide)s have been thoroughly investigated. Results Phase transition temperature dependence on the molecular weight and hydrophilic/hydrophobic ratio in the polymers were observed in water. Biological test results showed that the obtained materials, both in disordered and micellar form, are non-hemolytic, highly compatible with fibroblasts, and toxic to glioblastoma cells. It was found that the polymer termini dictates the mode of action of the system. Conclusion The cholesteryl moiety acts as a cell-penetrating agent, which enables disruption of the plasma membrane and in effect leads to the restriction of the tumor growth. Cholesterol end-capped PNIPAAm showing in vitro anticancer efficacy can be developed not only as drug carriers but also as components of combined/synergistic therapy.
- Published
- 2020
9. Multilayer Films Based on Chitosan/Pectin Polyelectrolyte Complexes as Novel Platforms for Buccal Administration of Clotrimazole
- Author
-
Anna Basa, Eliza Wolska, Katarzyna Winnicka, Izabela Kurowska, Magdalena Wróblewska, Joanna Potaś, Agnieszka Z. Wilczewska, Mateusz Maciejczyk, and Emilia Szymańska
- Subjects
food.ingredient ,Pectin ,Pharmaceutical Science ,polyelectrolyte complex ,Dosage form ,Article ,clotrimazole ,Chitosan ,chemistry.chemical_compound ,food ,Pharmacy and materia medica ,medicine ,Mucoadhesion ,oral candidiasis ,Fourier transform infrared spectroscopy ,pectin ,Clotrimazole ,Buccal administration ,Combinatorial chemistry ,Polyelectrolyte ,RS1-441 ,chemistry ,multilayer film ,chitosan ,buccal delivery ,medicine.drug - Abstract
Buccal films are recognized as easily applicable, microbiologically stable drug dosage forms with good retentivity at the mucosa intended for the therapy of oromucosal conditions, especially infectious diseases. Multilayer films composed of layers of oppositely charged polymers separated by ionically interacting polymeric chains creating polyelectrolyte complexes represent very interesting and relatively poorly explored area. We aimed to develop the antifungal multilayer systems composed of cationic chitosan and anionic pectin as potential platforms for controlled delivery of clotrimazole. The systems were pharmaceutically characterized with regard to inter alia their release kinetics under different pH conditions, physicomechanical, or mucoadhesion properties with using an animal model of the buccal mucosa. The antifungal activity against selected Candida sp. and potential cytotoxicity with regard to human gingival fibroblasts were also evaluated. Interactions between polyions were characterized with Fourier transform infrared spectroscopy. Different clotrimazole distribution in the films layers highly affected their in vitro dissolution profile. The designed films were recognized as intelligent pH-responsive systems with strong antifungal effect and satisfactory safety profile. As addition of chitosan resulted in the improved antifungal behavior of the drug, the potential utilization of the films in resistant cases of oral candidiasis might be worth of further exploration.
- Published
- 2021
- Full Text
- View/download PDF
10. Membrane-active diacylglycerol-terminated thermoresponsive polymers: RAFT synthesis and biocompatibility evaluation
- Author
-
Izabela Kurowska, Karolina H. Markiewicz, Katarzyna Niemirowicz-Laskowska, Paweł Misiak, Mathias Destarac, Przemysław Wielgat, Iwona Misztalewska-Turkowicz, Gabriela Siemiaszko, Halina Car, Agnieszka Z. Wilczewska, Interactions moléculaires et réactivité chimique et photochimique (IMRCP), Institut de Chimie de Toulouse (ICT), Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Université de Toulouse (UT)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université de Toulouse (UT)-Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Institut Ecologie et Environnement (INEE), Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS)-Fédération de Recherche Fluides, Energie, Réacteurs, Matériaux et Transferts (FERMAT), Institut National des Sciences Appliquées - Toulouse (INSA Toulouse), Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Centre National de la Recherche Scientifique (CNRS)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université de Toulouse (UT)-Institut National des Sciences Appliquées - Toulouse (INSA Toulouse), Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Institut National des Sciences Appliquées (INSA)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS), P3R - Polymères de Précision par Procédés Radicalaires (P3R), Institut National des Sciences Appliquées (INSA)-Université de Toulouse (UT)-Institut National des Sciences Appliquées (INSA)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie de Toulouse (ICT), Laboratoire de synthèse organique (DCSO), and École polytechnique (X)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
- Subjects
Polymers and Plastics ,Organic Chemistry ,Materials Chemistry ,[CHIM]Chemical Sciences ,General Physics and Astronomy - Abstract
International audience
- Published
- 2022
11. Evaluation of Cytotoxic Effect of Cholesterol End-Capped Poly(
- Author
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Pawel, Misiak, Katarzyna, Niemirowicz-Laskowska, Karolina H, Markiewicz, Iwona, Misztalewska-Turkowicz, Przemysław, Wielgat, Izabela, Kurowska, Gabriela, Siemiaszko, Mathias, Destarac, Halina, Car, and Agnieszka Z, Wilczewska
- Subjects
Adult ,Drug Carriers ,Polymers ,Acrylic Resins ,Temperature ,Water ,thermoresponsive polymer micelles ,Antineoplastic Agents ,Fibroblasts ,cell-penetrating molecules ,drug carriers ,Hemolysis ,Phase Transition ,Polymerization ,Molecular Weight ,cholesterol-end capped poly(N-isopropylacrylamide) ,Mice ,Cholesterol ,Cell Line, Tumor ,Animals ,Humans ,Glioblastoma ,Hydrophobic and Hydrophilic Interactions ,Micelles ,Original Research - Abstract
Purpose Efficient intracellular delivery of a therapeutic compound is an important feature of smart drug delivery systems (SDDS). Modification of a carrier structure with a cell-penetrating ligand, ie, cholesterol moiety, is a strategy to improve cellular uptake. Cholesterol end-capped poly(N-isopropylacrylamide)s offer a promising foundation for the design of efficient thermoresponsive drug delivery systems. Methods A series of cholesterol end-capped poly(N-isopropylacrylamide)s (PNIPAAm) with number-average molar masses ranging from 3200 to 11000 g·mol–1 were synthesized by reversible addition-fragmentation chain transfer (RAFT) polymerization from original xanthate-functionalized cholesterol and self-assembled into micelles. The physicochemical characteristics and cytotoxicity of cholesterol end-capped poly(N-isopropylacrylamide)s have been thoroughly investigated. Results Phase transition temperature dependence on the molecular weight and hydrophilic/hydrophobic ratio in the polymers were observed in water. Biological test results showed that the obtained materials, both in disordered and micellar form, are non-hemolytic, highly compatible with fibroblasts, and toxic to glioblastoma cells. It was found that the polymer termini dictates the mode of action of the system. Conclusion The cholesteryl moiety acts as a cell-penetrating agent, which enables disruption of the plasma membrane and in effect leads to the restriction of the tumor growth. Cholesterol end-capped PNIPAAm showing in vitro anticancer efficacy can be developed not only as drug carriers but also as components of combined/synergistic therapy.
- Published
- 2020
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