Acetal-Linked Paclitaxel Polymeric Prodrug Based on Functionalized mPEG-PCL Diblock Polymer for pH-Triggered Drug Delivery
| Autor: | Xing Zhou, Ronghua Song, Chao Ma, Xueyao Hu, Yanhao Deng, Wei Sun, Yinglei Zhai, Lina Jia |
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| Rok vydání: | 2017 |
| Předmět: |
Polymers and Plastics
acetal 02 engineering and technology 010402 general chemistry 01 natural sciences Micelle Article prodrug polymer micelles pH-sensitive paclitaxel lcsh:QD241-441 chemistry.chemical_compound lcsh:Organic chemistry medicine Doxorubicin Acetal General Chemistry Prodrug 021001 nanoscience & nanotechnology Combinatorial chemistry In vitro 0104 chemical sciences Paclitaxel chemistry Drug delivery 0210 nano-technology Ethylene glycol medicine.drug |
| Zdroj: | Polymers; Volume 9; Issue 12; Pages: 698 Polymers Polymers, Vol 9, Iss 12, p 698 (2017) |
| ISSN: | 2073-4360 |
| Popis: | The differences in micro-environment between cancer cells and the normal ones offer the possibility to develop stimuli-responsive drug-delivery systems for overcoming the drawbacks in the clinical use of anticancer drugs, such as paclitaxel, doxorubicin, and etc. Hence, we developed a novel endosomal pH-sensitive paclitaxel (PTX) prodrug micelles based on functionalized poly(ethylene glycol)-poly(ε-caprolactone) (mPEG-PCL) diblock polymer with an acid-cleavable acetal (Ace) linkage (mPEG-PCL-Ace-PTX). The mPEG-PCL-Ace-PTX5 with a high drug content of 23.5 wt % was self-assembled in phosphate buffer (pH 7.4, 10 mM) into nanosized micelles with an average diameter of 68.5 nm. The in vitro release studies demonstrated that mPEG-PCL-Ace-PTX5 micelles was highly pH-sensitive, in which 16.8%, 32.8%, and 48.2% of parent free PTX was released from mPEG-PCL-Ace-PTX5 micelles in 48 h at pH 7.4, 6.0, and 5.0, respectively. Thiazolyl Blue Tetrazolium Bromide (MTT) assays suggested that the pH-sensitive PTX prodrug micelles displayed higher therapeutic efficacy against MCF-7 cells compared with free PTX. Therefore, the PTX prodrug micelles with acetal bond may offer a promising strategy for cancer therapy. |
| Databáze: | OpenAIRE |
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