pH-Sensitive degradable polymersomes for triggered release of anticancer drugs: A comparative study with micelles
Abstract
pH-Sensitive degradable polymersomes and micelles were prepared based on diblock copolymer of poly(ethylene glycol) (PEG) and an acid-labile polycarbonate, poly(2,4,6-trimethoxybenzylidenepentaerythritol carbonate) (PTMBPEC). Polymersomes of PEG(1.9k)-PTMBPEC(6k) revealed average sizes of 100-200 nm. The acetals of polymersomes, similar to those of PEG(5k)-PTMBPEC(5.8k) micelles, though stable at pH 7.4 were prone to fast hydrolysis at mildly acidic pH of 4.0 and 5.0, with half lives of 0.5 and 3d, respectively. The acetal hydrolysis resulted in significant size increase of polymersomes, to over 1000 nm in 24h at pH 4.0. Drug encapsulation studies revealed that polymersomes were able to simultaneously load paclitaxel (PTX, hydrophobic) and doxorubicin hydrochloride (DOX.HCl, hydrophilic), whereas micelles loaded PTX only. Notably, polymersomes showed lower drug loading efficiencies for PTX than micelles (30.0-37.7% versus 61.4-65.2%). The in vitro release studies demonstrated that release of PTX and DOX.HCl from polymersomes was highly pH-dependent, i.e. significantly faster drug release at mildly acidic pH of 4.0 and 5.0 compared to physiological pH. Furthermore, much higher release rates were observed for PTX release from the polymersomes compared to that from the micelles under otherwise the same conditions. These pH-sensitive nano-sized degradable polymersomes hold great promise for combination therapy for cancers.
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The size of micelle increased from 150 nm to about 400 nm in 3 h, reaching over 1000 nm after 12 h at pH 4.0.
“The size of micelle increased from 150 nm to about 400 nm in 3 h, reaching over 1000 nm after 12 h.”
From Recent Advances in Nanomicelles Delivery Systems. (2020) · cites this paper as [142]
In vitro release studies displayed a remarkably faster release of paclitaxel and DOX at pH 4.0 and 5.0 than at pH 7.4.
“In vitro release studies displayed a remarkably faster release of paclitaxel and DOX at pH 4.0 and 5.0 than at pH 7.4.”
From Recent Advances in Nanomicelles Delivery Systems. (2020) · cites this paper as [142]
Under the acidic pH environment, the acetal hydrolysis resulted in strong micelles swelling, because of decreasing the hydrophobicity of the hydrophobic part.
“Under the acidic pH environment, the acetal hydrolysis resulted in strong micelles swelling, because of decreasing the hydrophobicity of the hydrophobic part.”
From Recent Advances in Nanomicelles Delivery Systems. (2020) · cites this paper as [142]
Cites
Polymersomes: Tough Vesicles Made from Diblock Copolymers
Discher, B. M., Won, Y., Ege, D. S., Lee, J. C., Bates, F. S., Discher, D. E., & Hammer, D. A. (1999) · Science · doi:10.1126/science.284.5417.1143 · Cited by 2,513 · see citing works
Discher, D., & Eisenberg, A. (2002) · Science · doi:10.1126/science.1074972 · Cited by 2,251 · see citing works
Stimuli-Responsive Polymersomes for Programmed Drug Delivery
Meng, F., Zhong, Z., & Feijén, J. (2009) · Biomacromolecules · doi:10.1021/bm801127d · Cited by 1,122 · see citing works
Self-citationTemporal targeting of tumour cells and neovasculature with a nanoscale delivery system
Sengupta, S., Eavarone, D. A., Capila, I., Zhao, G., Watson, N., Kiziltepe, T., & Sasisekharan, R. (2005) · Nature · doi:10.1038/nature03794 · Cited by 946 · see citing works
Oxidation-responsive polymeric vesicles
Napoli, A., Valentini, M., Tirelli, N., et al. (2004) · Nature Materials · doi:10.1038/nmat1081 · Cited by 889 · see citing works
Discher, D. E., & Ahmed, F. (2006) · Annual Review of Biomedical Engineering · doi:10.1146/annurev.bioeng.8.061505.095838 · Cited by 844 · see citing works
Giant Wormlike Rubber Micelles
Won, Y., DAVIS, H. T., & Bates, F. S. (1999) · Science · doi:10.1126/science.283.5404.960 · Cited by 671 · see citing works
Self-porating polymersomes of peg–pla and peg–pcl: Hydrolysis-triggered controlled release vesicles
Ahmed, F., & Discher, D. E. (2004) · Journal of Controlled Release · doi:10.1016/j.jconrel.2003.12.021 · Cited by 667 · see citing works
pH-Sensitive Vesicles Based on a Biocompatible Zwitterionic Diblock Copolymer
Du, J., Tang, Y., Lewis, A. L., & Armes, S. P. (2005) · Journal of the American Chemical Society · doi:10.1021/ja056514l · Cited by 603 · see citing works
pH-Responsive Copolymer Assemblies for Controlled Release of Doxorubicin
Gillies, E. R., & Fréchet, J. M. J. (2005) · Bioconjugate Chemistry · doi:10.1021/bc049851c · Cited by 551 · see citing works
Ahmed, F., Pakunlu, R. I., Brannan, A. K., Bates, F. S., Minko, T., & Discher, D. E. (2006) · Journal of Controlled Release · doi:10.1016/j.jconrel.2006.07.012 · Cited by 548 · see citing works
Polymeric anticancer drugs with pH-controlled activation
Ulbrich, K. (2004) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2003.10.040 · Cited by 495 · see citing works
Rijcken, C. J. F., Soga, O., Hennink, W. E., & van Nostrum, C. F. (2007) · Journal of Controlled Release · doi:10.1016/j.jconrel.2007.03.023 · Cited by 487 · see citing works
Qin, S., Geng, Y., Discher, D. E., et al. (2006) · Advanced Materials · doi:10.1002/adma.200601019 · Cited by 478 · see citing works
Acetal-Derivatized Dextran: An Acid-Responsive Biodegradable Material for Therapeutic Applications
Bachelder, E. M., Beaudette, T. T., Broaders, K. E., Dashe, J., & Fréchet, J. M. J. (2008) · Journal of the American Chemical Society · doi:10.1021/ja803947s · Cited by 475 · see citing works
Stimuli-responsive polymer vesicles
Li, M., & Keller, P. (2009) · Soft Matter · doi:10.1039/b815725a · Cited by 466 · see citing works
Biomimetic pH Sensitive Polymersomes for Efficient DNA Encapsulation and Delivery
Lomas, H., Cantón, I., MacNeil, S., Du, J., Armes, S. P., Ryan, A. J., Lewis, A. L., & Battaglia, G. (2007) · Advanced Materials · doi:10.1002/adma.200700941 · Cited by 449 · see citing works
Polymerized ABA Triblock Copolymer Vesicles
Nardin, C., Hirt, T. D., Leukel, J., & Meier, W. P. (1999) · Langmuir · doi:10.1021/la990951u · Cited by 434 · see citing works
Emerging applications of polymersomes in delivery: From molecular dynamics to shrinkage of tumors
Discher, D. E., Ortiz, V., Srinivas, G., Klein, M. L., Kim, Y., Christian, D. A., Cai, S., Photos, P. J., & Ahmed, F. (2007) · Progress in Polymer Science · doi:10.1016/j.progpolymsci.2007.05.011 · Cited by 378 · see citing works
Holowka, E. P., Sun, V. Z., Kamei, D. T., et al. (2006) · Nature Materials · doi:10.1038/nmat1794 · Cited by 372 · see citing works
Polymersome carriers: From self-assembly to siRNA and protein therapeutics
Christian, D. A., Cai, S., Bowen, D. M., Kim, Y., Pajerowski, J. D., & Discher, D. E. (2008) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2008.09.025 · Cited by 372 · see citing works
Won, Y., Brannan, A. K., DAVIS, H. T., & Bates, F. S. (2002) · The Journal of Physical Chemistry B · doi:10.1021/jp013639d · Cited by 340 · see citing works
Acetals as pH-Sensitive Linkages for Drug Delivery
Gillies, E. R., Goodwin, A. P., & Fréchet, J. M. J. (2004) · Bioconjugate Chemistry · doi:10.1021/bc049853x · Cited by 332 · see citing works
Preparation and brain delivery property of biodegradable polymersomes conjugated with ox26
Pang, Z., Lu, W., Gao, H., Hu, K., Chen, J., Zhang, C., Gao, X., Jiang, X., & Zhu, C. (2008) · Journal of Controlled Release · doi:10.1016/j.jconrel.2008.03.007 · Cited by 264 · see citing works
A new approach towards acid sensitive copolymer micelles for drug delivery
Gillies, E. R., & Fréchet, J. M. J. (2003) · Chemical Communications · doi:10.1039/b304251k · Cited by 252 · see citing works
Chen, W., Meng, F., Li, F., Ji, S., & Zhong, Z. (2009) · Biomacromolecules · doi:10.1021/bm900074d · Cited by 241 · see citing works
Self-citationDou, H., Jiang, M., Peng, H., et al. (2003) · Angewandte Chemie International Edition · doi:10.1002/anie.200250254 · Cited by 237 · see citing works
Biodegradable polymersomes as a basis for artificial cells: Encapsulation, release and targeting
Meng, F., Engbers, G. H. M., & Feijen, J. (2005) · Journal of Controlled Release · doi:10.1016/j.jconrel.2004.09.026 · Cited by 227 · see citing works
Self-citationMurthy, N., Campbell, J. S., Fausto, N., Hoffman, A. S., & Stayton, P. S. (2003) · Journal of Controlled Release · doi:10.1016/s0168-3659(03)00099-3 · Cited by 221 · see citing works
Wiradharma, N., Tong, Y. W., & Yang, Y. (2009) · Biomaterials · doi:10.1016/j.biomaterials.2009.03.006 · Cited by 204 · see citing works
Gasparini, G., Longo, R., Fanelli, M., & Teicher, B. A. (2005) · Journal of Clinical Oncology · doi:10.1200/jco.2005.10.022 · Cited by 201 · see citing works
Polymer Therapeutics Designed for a Combination Therapy of Hormone‐Dependent Cancer
Vicent, M. J., Greco, F., Nicholson, R. I., Paul, A., Griffiths, P. C., & Duncan, R. (2005) · Angewandte Chemie International Edition · doi:10.1002/anie.200462960 · Cited by 199 · see citing works
Polymersome delivery of siRNA and antisense oligonucleotides
Kim, Y.-H., Tewari, M., Pajerowski, J. D., Cai, S., Sen, S., Williams, J. H., Sirsi, S. R., Lutz, G. J., & Discher, D. E. (2008) · Journal of Controlled Release · doi:10.1016/j.jconrel.2008.10.020 · Cited by 185 · see citing works
Fully Acid-Degradable Biocompatible Polyacetal Microparticles for Drug Delivery
Paramonov, S. E., Bachelder, E. M., Beaudette, T. T., et al. (2008) · Bioconjugate Chemistry · doi:10.1021/bc7004472 · Cited by 178 · see citing works
Bae, Y., Diezi, T. A., Zhao, A., & Kwon, G. S. (2007) · Journal of Controlled Release · doi:10.1016/j.jconrel.2007.05.038 · Cited by 173 · see citing works
Meng, F., Hiemstra, C., Engbers, G. H. M., & Feijén, J. (2003) · Macromolecules · doi:10.1021/ma034040+ · Cited by 169 · see citing works
Self-citationpH-Induced Release from P2VP−PEO Block Copolymer Vesicles
Borchert, U., Lipprandt, U., Bilang, M., Kimpfler, A., Rank, A., Peschka‐Süss, R., Schubert, R., Lindner, P., & Förster, S. (2006) · Langmuir · doi:10.1021/la060227t · Cited by 163 · see citing works
Soft Vesicles Formed by Diblock Codendrimers of Poly(benzyl ether) and Poly(methallyl dichloride)
Yang, M., Wang, W., Yuan, F., et al. (2005) · Journal of the American Chemical Society · doi:10.1021/ja052713t · Cited by 149 · see citing works
Sacchi, A., Gasparri, A. M., Gallo‐Stampino, C., Toma, S., Curnis, F., & Corti, A. (2006) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-05-1147 · Cited by 144 · see citing works
Synthesis and Degradation of pH-Sensitive Linear Poly(amidoamine)s
Jain, R., Standley, S. M., & Fréchet, J. M. J. (2007) · Macromolecules · doi:10.1021/ma062319v · Cited by 139 · see citing works
Real‐Time Membrane Fission of Giant Polymer Vesicles
Zhou, Y., & Yan, D. (2005) · Angewandte Chemie International Edition · doi:10.1002/anie.200462622 · Cited by 116 · see citing works
Acid-cleavable polymeric core–shell particles for delivery of hydrophobic drugs
Chan, Y., Bulmuş, V., Zareie, M. H., Byrne, F. L., Barner, L., & Kavallaris, M. (2006) · Journal of Controlled Release · doi:10.1016/j.jconrel.2006.07.025 · Cited by 94 · see citing works
VANDENBERG, E. J., & Tian, D. (1999) · Macromolecules · doi:10.1021/ma9816822 · Cited by 84 · see citing works
Harasym, T. O., Tardi, P. G., Harasym, N. L., Harvie, P., Johnstone, S. A., & Mayer, L. D. (2006) · Oncology Research Featuring Preclinical and Clinical Cancer Therapeutics · doi:10.3727/000000006783980937 · Cited by 84 · see citing works
Lee, H. J., Yang, S. R., An, E. J., & Kim, J.-D. (2006) · Macromolecules · doi:10.1021/ma060198t · Cited by 77 · see citing works
Flagged first, then by citations
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Sorted by citations
pH-Sensitive nano-systems for drug delivery in cancer therapy
Liu, J., Huang, Y., Kumar, A., Tan, A., Jin, S., Mozhi, A., & Liang, X.-J. (2014) · Biotechnology Advances · doi:10.1016/j.biotechadv.2013.11.009 · Cited by 1,121 · see citing works
pH- and ion-sensitive polymers for drug delivery
Yoshida, T., Lai, T. C., Kwon, G. S., & Sako, K. (2013) · Expert Opinion on Drug Delivery · doi:10.1517/17425247.2013.821978 · Cited by 367 · see citing works
Tempelaar, S., Mespouille, L., Coulembier, O., Dubois, P., & Dove, A. P. (2013) · Chem. Soc. Rev. · doi:10.1039/c2cs35268k · Cited by 345 · see citing works
Gu, Y., Zhong, Y., Meng, F., Cheng, R., Deng, C., & Zhong, Z. (2013) · Biomacromolecules · doi:10.1021/bm400615n · Cited by 187 · see citing works
Self-citationRational Design of Biomaterials to Potentiate Cancer Thermal Therapy
Zhu, Y., Li, Q., Wang, C., Hao, Y., Yang, N., Chen, M., Ji, J., Feng, L., & Liu, Z. (2023) · Chemical Reviews · doi:10.1021/acs.chemrev.2c00822 · Cited by 163 · see citing works
Liu, R., Li, D., He, B., Xu, X., Sheng, M., Lai, Y., Wang, G., & Gu, Z. (2011) · Journal of Controlled Release · doi:10.1016/j.jconrel.2011.02.031 · Cited by 157 · see citing works
Recent Advances in Nanomicelles Delivery Systems.
Tawfik, S. M., Azizov, S., Elmasry, M. R., Sharipov, M., & Lee, Y.-I. (2020) · Nanomaterials · doi:10.3390/nano11010070 · Cited by 156 · see citing works
“Zhong and coworkers studied the synthesis of pH-sensitive biodegradable micelles, which were designed from the block copolymers PEG-PTMBPEC [142].”
BackgroundA review of polypeptide-based polymersomes
Zhao, L., Li, N., Wang, K., Shi, C., Zhang, L., & Luan, Y. (2014) · Biomaterials · doi:10.1016/j.biomaterials.2013.10.063 · Cited by 149 · see citing works
Li, L., Wang, J., Kong, H., Zeng, Y., & Liu, G. (2018) · Science and Technology of Advanced Materials · doi:10.1080/14686996.2018.1528850 · Cited by 71 · see citing works
- Authors
- Chen, W., Meng, F., Cheng, R., & Zhong, Z.
- Affiliations
- Soochow University (CN)
- Corresponding author
- Meng, Fenghua
- Zhong, Zhiyuan
- Venue
- Journal of Controlled Release
- Publisher
- Elsevier BV
- Published
- 2010-02
- Volume
- 142
- Issue
- 1
- Pages
- 40-46
- ISSN
- 0168-3659 (ISSN-L)
- OpenAlex
- W2053613167
- Cited by
- 458
- References
- 45
- Citations by year
- 2026: 6 · 2025: 8 · 2024: 15 · 2023: 17 · 2022: 19 · 2021: 21 · 2020: 34 · 2019: 25 · 2018: 29 · 2017: 25 · 2016: 35 · 2015: 52 · 2014: 42 · 2013: 40 · 2012: 42
- FWCI
- 13.17
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Controlled Release (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Natural Science Foundation of China
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Physical Sciences › Materials Science › Polymers and Plastics › Dendrimers and Hyperbranched Polymers
- Keywords
- polymersomes, micelles, pH-responsive drug delivery, degradable polymers, acetal hydrolysis, paclitaxel, doxorubicin, combination cancer therapy, encapsulation efficiency, pH-dependent drug release, nanocarriers
- MeSH terms
- Acetals, Antineoplastic Agents, Cell Line, Cell Survival, Delayed-Action Preparations, Doxorubicin, HeLa Cells, Humans, Hydrogen-Ion Concentration, Hydrolysis, Micelles, Particle Size, Polycarboxylate Cement, Polyethylene Glycols, Paclitaxel
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