Unknown

Dataset Information

0

Self-Assembled Redox Dual-Responsive Prodrug-Nanosystem Formed by Single Thioether-Bridged Paclitaxel-Fatty Acid Conjugate for Cancer Chemotherapy.


ABSTRACT: 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.

SUBMITTER: Luo C 

PROVIDER: S-EPMC5541379 | biostudies-literature | 2016 Sep

REPOSITORIES: biostudies-literature

altmetric image

Publications

Self-Assembled Redox Dual-Responsive Prodrug-Nanosystem Formed by Single Thioether-Bridged Paclitaxel-Fatty Acid Conjugate for Cancer Chemotherapy.

Luo Cong C   Sun Jin J   Liu Dan D   Sun Bingjun B   Miao Lei L   Musetti Sara S   Li Jing J   Han Xiaopeng X   Du Yuqian Y   Li Lin L   Huang Leaf L   He Zhonggui Z  

Nano letters 20160808 9


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-heterogen  ...[more]

Similar Datasets

| S-EPMC8241199 | biostudies-literature
| S-EPMC6719549 | biostudies-literature
| S-EPMC7023610 | biostudies-literature
| S-EPMC5767894 | biostudies-other
| S-EPMC4486357 | biostudies-literature
| S-EPMC7760941 | biostudies-literature
| S-EPMC6709549 | biostudies-literature
| S-EPMC3207205 | biostudies-literature
| S-EPMC5525542 | biostudies-literature
| S-EPMC8343193 | biostudies-literature