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Self-Assembled Redox Dual-Responsive Prodrug-Nanosystem Formed by Single Thioether-Bridged Paclitaxel-Fatty Acid Conjugate for Cancer Chemotherapy
Open accessAbstract
Chemotherapeutic efficacy can be greatly improved by developing nanoparticulate drug delivery systems (nano-DDS) with high drug loading capacity and smart stimulus-triggered drug release in tumor cells. Herein, we report a novel redox dual-responsive prodrug-nanosystem self-assembled by hydrophobic small-molecule conjugates of paclitaxel (PTX) and oleic acid (OA). Thioether linked conjugates (PTX-S-OA) and dithioether inserted conjugates (PTX-2S-OA) are designed to respond to the redox-heterogeneity in tumor. Dithioether has been reported to show redox dual-responsiveness, but we find that PTX-S-OA exhibits superior redox sensitivity over PTX-2S-OA, achieving more rapid and selective release of free PTX from the prodrug nanoassemblies triggered by redox stimuli. PEGylated PTX-S-OA nanoassemblies, with impressively high drug loading (57.4%), exhibit potent antitumor activity in a human epidermoid carcinoma xenograft. This novel prodrug-nanosystem addresses concerns related to the low drug loading and inefficient drug release from hydrophobic prodrugs of PTX, and provides possibilities for the development of redox dual-sensitive conjugates or polymers for efficient anticancer drug delivery.
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Li, C., Wang, J., Wang, Y., Gao, H., Wei, G., Huang, Y., Yu, H., Gan, Y., Wang, Y., Mei, L., et al. (2019) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2019.08.003 · Cited by 818
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Self-citationInternal stimuli-responsive nanocarriers for drug delivery: Design strategies and applications
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Metadata
- Authors
- Luo, C., Sun, J., Liu, D., Sun, B., Miao, L., Musetti, S., Li, J., Han, X., Du, Y., Li, L., Huang, L., & He, Z.
- Venue
- Nano Letters
- Publisher
- American Chemical Society (ACS)
- Published
- 2016-08-08
- Volume
- 16
- Issue
- 9
- Pages
- 5401-5408
- ISSN
- 1530-6984 (ISSN-L)
- 1530-6992
- OpenAlex
- W2503470809
- Cited by
- 443
- References
- 0
- FWCI
- 15.54
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: Self-Assembled Redox Dual-Responsive Prodrug-Nanosystem Formed by Single Thioether-Bridged Paclitaxel-Fatty Acid Conjugate for Cancer Chemotherapy. https://app.cochat.ai/papers/10.1021/acs.nanolett.6b01632
- The paper
- Luo, C., Sun, J., Liu, D., Sun, B., Miao, L., Musetti, S., Li, J., Han, X., Du, Y., Li, L., Huang, L., & He, Z. (2016). Self-Assembled Redox Dual-Responsive Prodrug-Nanosystem Formed by Single Thioether-Bridged Paclitaxel-Fatty Acid Conjugate for Cancer Chemotherapy. Nano Letters. https://doi.org/10.1021/acs.nanolett.6b01632
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