Oral Delivery of DMAB-Modified Docetaxel-Loaded PLGA-TPGS Nanoparticles for Cancer Chemotherapy.
Oral Delivery of DMAB-Modified Docetaxel-Loaded PLGA-TPGS Nanoparticles for Cancer Chemotherapy.
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用于癌症化疗的 DMAB 修饰多西他赛负载 PLGA-TPGS 纳米颗粒的口服给药
DOI：
10.1007/s11671-010-9741-8
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发表时间：
2011-12
影响因子：
--
通讯作者：
Huang, Laiqiang
中科院分区：
文献类型：
--
作者：
Chen, Hongbo;Zheng, Yi;Tian, Ge;Tian, Yan;Zeng, Xiaowei;Liu, Gan;Liu, Kexin;Li, Lei;Li, Zhen;Mei, Lin;Huang, Laiqiang
本研究以可生物降解的PLGA-TPGS无规共聚物为原料，制备了三种不同的纳米粒，包括DMAB修饰的PLGA纳米粒、未修饰的PLGA-TPGS纳米粒和DMAB修饰的PLGA-TPGS纳米粒。首先，合成并表征了PLGA-TPGS无规共聚物。DMAB用于增加在细胞表面的保留时间，从而增加颗粒摄取的机会并提高口服药物的生物利用度。发现纳米颗粒为球形，平均粒径为约250 nm。经DMAB修饰后，PLGA-TPGS纳米粒表面电荷变为正电荷。结果还显示，DMAB修饰的PLGA-TPGS纳米粒具有显著高于DMAB修饰的PLGA纳米粒和未修饰的PLGA-TPGS纳米粒的细胞摄取水平。在体外，细胞毒性实验显示，就针对MCF-7细胞的细胞毒性而言，DMAB修饰的PLGA-TPGS纳米颗粒制剂优于商业泰索帝®。总之，通过DMAB修饰的PLGA-TPGS纳米颗粒制剂的口服化疗是对患者有吸引力和有前途的治疗选择。
Three types of nanoparticle formulation from biodegradable PLGA-TPGS random copolymer were developed in this research for oral administration of anticancer drugs, which include DMAB-modified PLGA nanoparticles, unmodified PLGA-TPGS nanoparticles and DMAB-modified PLGA-TPGS nanoparticles. Firstly, the PLGA-TPGS random copolymer was synthesized and characterized. DMAB was used to increase retention time at the cell surface, thus increasing the chances of particle uptake and improving oral drug bioavailability. Nanoparticles were found to be of spherical shape with an average particle diameter of around 250 nm. The surface charge of PLGA-TPGS nanoparticles was changed to positive after DMAB modification. The results also showed that the DMAB-modified PLGA-TPGS nanoparticles have significantly higher level of the cellular uptake than that of DMAB-modified PLGA nanoparticles and unmodified PLGA-TPGS nanoparticles. In vitro, cytotoxicity experiment showed advantages of the DMAB-modified PLGA-TPGS nanoparticle formulation over commercial Taxotere®in terms of cytotoxicity against MCF-7 cells. In conclusion, oral chemotherapy by DMAB-modified PLGA-TPGS nanoparticle formulation is an attractive and promising treatment option for patients.
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影响因子：
--
作者：
Mei L;Zhang Y;Zheng Y;Tian G;Song C;Yang D;Chen H;Sun H;Tian Y;Liu K;Li Z;Huang L
通讯作者：
Huang L
影响因子：
3.2
作者：
Nabholtz, J M;Tonkin, K;Mackey, J
通讯作者：
Mackey, J
影响因子：
5.8
作者：
Pandey, R;Ahmad, Z;Khuller, GK
通讯作者：
Khuller, GK
DOI：
10.1016/j.ddtec.2005.05.019
发表时间：
2005-01-01
期刊：
Drug discovery today. Technologies
影响因子：
--
作者：
Florence, Alexander T
通讯作者：
Florence, Alexander T
影响因子：
45.3
作者：
Malingré, MM;Richel, DJ;Schellens, JHM
通讯作者：
Schellens, JHM