Fabrication of Conjugated Amphiphilic Triblock Copolymer for Drug Delivery and Fluorescence Cell Imaging
Abstract
An elegant integration of light-emitting segments into the structure of polymeric delivery systems endows the resulting self-assembled nanovehicles with the diagnostic ability toward an enhanced therapeutic efficiency. A variety of polyfluorene (PF)-based binary delivery systems were designed and developed successfully, but PF-based ternary formulations remain rarely explored, likely due to the synthetic challenge. To develop a universal synthesis strategy toward linear conjugated amphiphilic triblock copolymer for cancer theranostics, herein we focused on the functionalization of the PF terminus for further chain extension and prepared well-defined PF-based amphiphilic triblock copolymers, PF- b -poly(ε-caprolactone)- b -poly(oligo(ethylene glycol) monomethyl ether methacrylate) (PF- b -PCL- b -POEGMA), by integrated state-of-the-art polymer chemistry techniques, including Suzuki reaction, ring-opening polymerization, atom transfer radical polymerization, and click coupling. The resulting conjugated amphiphilic triblock copolymers can self-assembe into core–shell-corona (CSC) micelles with PF block constructing the inner hydrophobic core for fluorescent tracking, PCL segment forming the hydrophobic middle shell for drug encapsulation, and POEGMA moiety building the hydrophilic outer corona for particulate stabilization. Interestingly, the CSC micelles with hydrophobic PCL middle layer show a greater drug loading capacity as well as a higher fluorescence quantum yield (Φ) relative to the core–shell micelles self-assembled from the control of PF- b -POEGMA diblock copolymers without PCL sequence due to having more hydrophobic spaces and better separation of PF sequence provided simultaneously by the PCL central block. The efficient cellular uptake of the anticancer drug doxorubicin-loaded CSC micelles together with the in vitro cytotoxicity against the HeLa cells makes the conjugated amphiphilic triblock copolymers developed herein a promising platform for simultaneous cell image and drug delivery, thus offering great potential for cancer theranostics.
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Wei's group developed novel amphiphilic copolymer-based nanomicelles with an average diameter of about 40 nm, a drug loading capacity of 70%, and a fluorescence quantum yield in water of Φ = 22%.
“Recently Wei’s group [78] have developed novel amphiphilic copolymer-based nanomicelles. The average diameter of these micelles was determined to be ~40 nm, which have demonstrated a relatively higher drug loading capacity of 70%. Moreover, authors have found that fluorescence quantum yield of micelles in water was higher, Φ = 22%.”
From Recent Advances in Nanomicelles Delivery Systems. (2020) · cites this paper as [78]
The IC50 of DOX-loaded nanomicelles against cancer cells was 68.59 μg/mL, while for DOX it was 2.33 μg/mL.
“Besides, the half-maximal inhibitory concentration (IC50) of DOX-loaded nanomicelles against cancer cells was found to be 68.59 μg/mL while for DOX it was found to be 2.33 μg/mL.”
From Recent Advances in Nanomicelles Delivery Systems. (2020) · cites this paper as [78]
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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
“Recently Wei’s group [78] have developed novel amphiphilic copolymer-based nanomicelles.”
Background
- Authors
- Zhao, X., Deng, K., Liu, F., Zhang, X., Yang, H., Peng, J., Liu, Z., Ma, L., Wang, B., & Wei, H.
- Affiliations
- State Key Laboratory of Applied Organic Chemistry (CN)
- Corresponding author
- Wei, Hua
- Venue
- ACS Biomaterials Science & Engineering
- Publisher
- American Chemical Society (ACS)
- Published
- 2018-01-23
- Volume
- 4
- Issue
- 2
- Pages
- 566-575
- ISSN
- 2373-9878 (ISSN-L)
- OpenAlex
- W2782012867
- Cited by
- 32
- References
- 44
- Citations by year
- 2026: 2 · 2025: 1 · 2024: 4 · 2023: 1 · 2022: 2 · 2021: 6 · 2020: 4 · 2019: 6 · 2018: 6
- FWCI
- 1.78
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- ACS Biomaterials Science & Engineering (publishedVersion)
- PubMed (publishedVersion)
- Lanzhou University Institutional Repository (submittedVersion)
- Funders
- Ministry of Education of the People's Republic of China (lzujbky-2016-ct05)
- National Natural Science Foundation of China (21504035, 51473072)
- Central People's Government of the People's Republic of China
- State Key Laboratory of Polymer Physics and Chemistry
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Physical Sciences › Chemistry › Organic Chemistry › Advanced Polymer Synthesis and Characterization
- Physical Sciences › Materials Science › Polymers and Plastics › Dendrimers and Hyperbranched Polymers
- Keywords
- polyfluorene, amphiphilic triblock copolymers, polycaprolactone, POEGMA, drug delivery, doxorubicin, cancer theranostics, self-assembly, Suzuki coupling, ring-opening polymerization, atom transfer radical polymerization, drug loading capacity, cellular uptake
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