pH-sensitive micelles self-assembled from polymer brush (PAE-g-cholesterol)-b-PEG-b-(PAE-g-cholesterol) for anticancer drug delivery and controlled release
Xiangxuan Huang,1 Wenbo Liao,1 Gang Zhang,1 Shimin Kang,1 Can Yang Zhang2 1School of Chemical Engineering and Energy Technology, Dongguan University of Technology, Dongguan, People’s Republic of China; 2Department of Pharmaceutical Sciences, College of Pharmacy, Washington State Universit...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Dove Medical Press
2017-03-01
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| Series: | International Journal of Nanomedicine |
| Subjects: | |
| Online Access: | https://www.dovepress.com/ph-sensitive-micelles-self-assembled-from-polymer-brush-pae-g-choleste-peer-reviewed-article-IJN |
| _version_ | 1818402703049490432 |
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| author | Huang X Liao W Zhang G Kang S Zhang CY |
| author_facet | Huang X Liao W Zhang G Kang S Zhang CY |
| author_sort | Huang X |
| collection | DOAJ |
| description | Xiangxuan Huang,1 Wenbo Liao,1 Gang Zhang,1 Shimin Kang,1 Can Yang Zhang2 1School of Chemical Engineering and Energy Technology, Dongguan University of Technology, Dongguan, People’s Republic of China; 2Department of Pharmaceutical Sciences, College of Pharmacy, Washington State University, Spokane, WA, USA Abstract: A novel amphiphilic pH-sensitive triblock polymer brush (poly(β-amino esters)-g-cholesterol)-b-poly(ethylene glycol)-b-(poly(β-amino esters)-g-cholesterol) ((PAE-g-Chol)-b-PEG-b-(PAE-g-Chol)) was designed and synthesized successfully through a three-step reaction, and their self-assembled polymeric micelles were used as hydrophobic anticancer drug delivery carriers to realize effectively controlled release. The critical micelle concentrations were 6.8 µg/mL, 12.6 µg/mL, 17.4 µg/mL, and 26.6 µg/mL at pH values of 7.4, 6.5, 6.0, and 5.0, respectively. The trend of critical micelle concentrations indicated that the polymer had high stability that could prolong the circulation time in the body. The hydrodynamic diameter and zeta potential of the polymeric micelles were influenced significantly by the pH values. As pH decreased from 7.4 to 5.0, the particle size and zeta potential increased from 205.4 nm to 285.7 nm and from +12.7 mV to +47.0 mV, respectively. The pKb of the polymer was confirmed to be approximately 6.5 by the acid–base titration method. The results showed that the polymer had sharp pH-sensitivity because of the protonation of the amino groups, resulting in transformation of the PAE segment from hydrophobic to hydrophilic. Doxorubicin-loaded polymeric micelles were prepared with a high loading content (20%) and entrapment efficiency (60%) using the dialysis method. The in vitro results demonstrated that drug release rate and cumulative release were obviously dependent on pH values. Furthermore, the drug release mechanism was also controlled by the pH values. The polymer had barely any cytotoxicity, whereas the doxorubicin-loaded system showed high toxicity for HepG2 cells as free drugs. All the results proved that the pH-sensitive triblock polymer brush and its self-assembled micelle might be a potential delivery carrier for anticancer drugs with sustained release. Keywords: pH-sensitive, micelle, anticancer, drug delivery, controlled release |
| first_indexed | 2024-12-14T08:12:34Z |
| format | Article |
| id | doaj.art-a1fac6a4b4a14664813fdad127e51144 |
| institution | Directory Open Access Journal |
| issn | 1178-2013 |
| language | English |
| last_indexed | 2024-12-14T08:12:34Z |
| publishDate | 2017-03-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | International Journal of Nanomedicine |
| spelling | doaj.art-a1fac6a4b4a14664813fdad127e511442022-12-21T23:10:02ZengDove Medical PressInternational Journal of Nanomedicine1178-20132017-03-01Volume 122215222631988pH-sensitive micelles self-assembled from polymer brush (PAE-g-cholesterol)-b-PEG-b-(PAE-g-cholesterol) for anticancer drug delivery and controlled releaseHuang XLiao WZhang GKang SZhang CYXiangxuan Huang,1 Wenbo Liao,1 Gang Zhang,1 Shimin Kang,1 Can Yang Zhang2 1School of Chemical Engineering and Energy Technology, Dongguan University of Technology, Dongguan, People’s Republic of China; 2Department of Pharmaceutical Sciences, College of Pharmacy, Washington State University, Spokane, WA, USA Abstract: A novel amphiphilic pH-sensitive triblock polymer brush (poly(β-amino esters)-g-cholesterol)-b-poly(ethylene glycol)-b-(poly(β-amino esters)-g-cholesterol) ((PAE-g-Chol)-b-PEG-b-(PAE-g-Chol)) was designed and synthesized successfully through a three-step reaction, and their self-assembled polymeric micelles were used as hydrophobic anticancer drug delivery carriers to realize effectively controlled release. The critical micelle concentrations were 6.8 µg/mL, 12.6 µg/mL, 17.4 µg/mL, and 26.6 µg/mL at pH values of 7.4, 6.5, 6.0, and 5.0, respectively. The trend of critical micelle concentrations indicated that the polymer had high stability that could prolong the circulation time in the body. The hydrodynamic diameter and zeta potential of the polymeric micelles were influenced significantly by the pH values. As pH decreased from 7.4 to 5.0, the particle size and zeta potential increased from 205.4 nm to 285.7 nm and from +12.7 mV to +47.0 mV, respectively. The pKb of the polymer was confirmed to be approximately 6.5 by the acid–base titration method. The results showed that the polymer had sharp pH-sensitivity because of the protonation of the amino groups, resulting in transformation of the PAE segment from hydrophobic to hydrophilic. Doxorubicin-loaded polymeric micelles were prepared with a high loading content (20%) and entrapment efficiency (60%) using the dialysis method. The in vitro results demonstrated that drug release rate and cumulative release were obviously dependent on pH values. Furthermore, the drug release mechanism was also controlled by the pH values. The polymer had barely any cytotoxicity, whereas the doxorubicin-loaded system showed high toxicity for HepG2 cells as free drugs. All the results proved that the pH-sensitive triblock polymer brush and its self-assembled micelle might be a potential delivery carrier for anticancer drugs with sustained release. Keywords: pH-sensitive, micelle, anticancer, drug delivery, controlled releasehttps://www.dovepress.com/ph-sensitive-micelles-self-assembled-from-polymer-brush-pae-g-choleste-peer-reviewed-article-IJNpH-sensitivemicelleanticancerdrug deliverycontrolled release |
| spellingShingle | Huang X Liao W Zhang G Kang S Zhang CY pH-sensitive micelles self-assembled from polymer brush (PAE-g-cholesterol)-b-PEG-b-(PAE-g-cholesterol) for anticancer drug delivery and controlled release International Journal of Nanomedicine pH-sensitive micelle anticancer drug delivery controlled release |
| title | pH-sensitive micelles self-assembled from polymer brush (PAE-g-cholesterol)-b-PEG-b-(PAE-g-cholesterol) for anticancer drug delivery and controlled release |
| title_full | pH-sensitive micelles self-assembled from polymer brush (PAE-g-cholesterol)-b-PEG-b-(PAE-g-cholesterol) for anticancer drug delivery and controlled release |
| title_fullStr | pH-sensitive micelles self-assembled from polymer brush (PAE-g-cholesterol)-b-PEG-b-(PAE-g-cholesterol) for anticancer drug delivery and controlled release |
| title_full_unstemmed | pH-sensitive micelles self-assembled from polymer brush (PAE-g-cholesterol)-b-PEG-b-(PAE-g-cholesterol) for anticancer drug delivery and controlled release |
| title_short | pH-sensitive micelles self-assembled from polymer brush (PAE-g-cholesterol)-b-PEG-b-(PAE-g-cholesterol) for anticancer drug delivery and controlled release |
| title_sort | ph sensitive micelles self assembled from polymer brush pae g cholesterol b peg b pae g cholesterol for anticancer drug delivery and controlled release |
| topic | pH-sensitive micelle anticancer drug delivery controlled release |
| url | https://www.dovepress.com/ph-sensitive-micelles-self-assembled-from-polymer-brush-pae-g-choleste-peer-reviewed-article-IJN |
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