Characterization and Therapeutic Effect of a pH Stimuli Responsive Polymeric Nanoformulation for Controlled Drug Release
Despite the large number of polymeric nanodelivery systems that have been recently developed, there is still room for improvement in terms of therapeutic efficiency. Most reported nanodevices for controlled release are based on drug encapsulation, which can lead to undesired drug leakage with a cons...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-06-01
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| Series: | Polymers |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2073-4360/12/6/1265 |
| _version_ | 1797566431119802368 |
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| author | Maria Victoria Cano-Cortes Jose Antonio Laz-Ruiz Juan Jose Diaz-Mochon Rosario Maria Sanchez-Martin |
| author_facet | Maria Victoria Cano-Cortes Jose Antonio Laz-Ruiz Juan Jose Diaz-Mochon Rosario Maria Sanchez-Martin |
| author_sort | Maria Victoria Cano-Cortes |
| collection | DOAJ |
| description | Despite the large number of polymeric nanodelivery systems that have been recently developed, there is still room for improvement in terms of therapeutic efficiency. Most reported nanodevices for controlled release are based on drug encapsulation, which can lead to undesired drug leakage with a consequent reduction in efficacy and an increase in systemic toxicity. Herein, we present a strategy for covalent drug conjugation to the nanodevice to overcome this drawback. In particular, we characterize and evaluate an effective therapeutic polymeric PEGylated nanosystem for controlled pH-sensitive drug release on a breast cancer (MDA-MB-231) and two lung cancer (A549 and H520) cell lines. A significant reduction in the required drug dose to reach its half maximal inhibitory concentration (IC50 value) was achieved by conjugation of the drug to the nanoparticles, which leads to an improvement in the therapeutic index by increasing the efficiency. The genotoxic effect of this nanodevice in cancer cells was confirmed by nucleus histone H2AX specific immunostaining. In summary, we successfully characterized and validated a pH responsive therapeutic polymeric nanodevice in vitro for controlled anticancer drug release. |
| first_indexed | 2024-03-10T19:26:42Z |
| format | Article |
| id | doaj.art-61858a57999c442fab0d3e589d91ece6 |
| institution | Directory Open Access Journal |
| issn | 2073-4360 |
| language | English |
| last_indexed | 2024-03-10T19:26:42Z |
| publishDate | 2020-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Polymers |
| spelling | doaj.art-61858a57999c442fab0d3e589d91ece62023-11-20T02:30:04ZengMDPI AGPolymers2073-43602020-06-01126126510.3390/polym12061265Characterization and Therapeutic Effect of a pH Stimuli Responsive Polymeric Nanoformulation for Controlled Drug ReleaseMaria Victoria Cano-Cortes0Jose Antonio Laz-Ruiz1Juan Jose Diaz-Mochon2Rosario Maria Sanchez-Martin3GENYO, Centre for Genomics and Oncological Research, Pfizer/University of Granada/Andalusian Regional Government, PTS Granada, Avda. Ilustración 114, 18016 Granada, SpainGENYO, Centre for Genomics and Oncological Research, Pfizer/University of Granada/Andalusian Regional Government, PTS Granada, Avda. Ilustración 114, 18016 Granada, SpainGENYO, Centre for Genomics and Oncological Research, Pfizer/University of Granada/Andalusian Regional Government, PTS Granada, Avda. Ilustración 114, 18016 Granada, SpainGENYO, Centre for Genomics and Oncological Research, Pfizer/University of Granada/Andalusian Regional Government, PTS Granada, Avda. Ilustración 114, 18016 Granada, SpainDespite the large number of polymeric nanodelivery systems that have been recently developed, there is still room for improvement in terms of therapeutic efficiency. Most reported nanodevices for controlled release are based on drug encapsulation, which can lead to undesired drug leakage with a consequent reduction in efficacy and an increase in systemic toxicity. Herein, we present a strategy for covalent drug conjugation to the nanodevice to overcome this drawback. In particular, we characterize and evaluate an effective therapeutic polymeric PEGylated nanosystem for controlled pH-sensitive drug release on a breast cancer (MDA-MB-231) and two lung cancer (A549 and H520) cell lines. A significant reduction in the required drug dose to reach its half maximal inhibitory concentration (IC50 value) was achieved by conjugation of the drug to the nanoparticles, which leads to an improvement in the therapeutic index by increasing the efficiency. The genotoxic effect of this nanodevice in cancer cells was confirmed by nucleus histone H2AX specific immunostaining. In summary, we successfully characterized and validated a pH responsive therapeutic polymeric nanodevice in vitro for controlled anticancer drug release.https://www.mdpi.com/2073-4360/12/6/1265covalent drug conjugationtherapeutic nanodevicepolymeric nanoparticlescancer therapycontrolled drug delivery |
| spellingShingle | Maria Victoria Cano-Cortes Jose Antonio Laz-Ruiz Juan Jose Diaz-Mochon Rosario Maria Sanchez-Martin Characterization and Therapeutic Effect of a pH Stimuli Responsive Polymeric Nanoformulation for Controlled Drug Release Polymers covalent drug conjugation therapeutic nanodevice polymeric nanoparticles cancer therapy controlled drug delivery |
| title | Characterization and Therapeutic Effect of a pH Stimuli Responsive Polymeric Nanoformulation for Controlled Drug Release |
| title_full | Characterization and Therapeutic Effect of a pH Stimuli Responsive Polymeric Nanoformulation for Controlled Drug Release |
| title_fullStr | Characterization and Therapeutic Effect of a pH Stimuli Responsive Polymeric Nanoformulation for Controlled Drug Release |
| title_full_unstemmed | Characterization and Therapeutic Effect of a pH Stimuli Responsive Polymeric Nanoformulation for Controlled Drug Release |
| title_short | Characterization and Therapeutic Effect of a pH Stimuli Responsive Polymeric Nanoformulation for Controlled Drug Release |
| title_sort | characterization and therapeutic effect of a ph stimuli responsive polymeric nanoformulation for controlled drug release |
| topic | covalent drug conjugation therapeutic nanodevice polymeric nanoparticles cancer therapy controlled drug delivery |
| url | https://www.mdpi.com/2073-4360/12/6/1265 |
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