Preparation of GST Inhibitor Nanoparticle Drug Delivery System and Its Reversal Effect on the Multidrug Resistance in Oral CarcinomaReportar como inadecuado


Preparation of GST Inhibitor Nanoparticle Drug Delivery System and Its Reversal Effect on the Multidrug Resistance in Oral Carcinoma


Preparation of GST Inhibitor Nanoparticle Drug Delivery System and Its Reversal Effect on the Multidrug Resistance in Oral Carcinoma - Descarga este documento en PDF. Documentación en PDF para descargar gratis. Disponible también para leer online.

1

School of Pharmaceutical Sciences, Jilin University, No.1266 Fujin Road, Changchun 130012, China

2

Changchun Women and Children Health Hospital, No. 962 Xinfa Road, Changchun 130061, China

3

School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, No.103 Wenhua Road, Shenyang 110016, China

4

China Japan Union Hospital, Jilin University, No. 126 Xiantai Street, Changchun 130033, China





*

Author to whom correspondence should be addressed.



Academic Editor: Luigi Pasqua

Abstract During the chemotherapy of cancer, drug resistance is the first issue that chemotherapeutic drugs cannot be effectively used for the treatment of cancers repeatedly for a long term, and the main reason for this is that tumor cell detoxification is mediated by GSH glutathione catalyzed by GST glutathione-S-transferase. In this study, a GST inhibitor, ethacrynic acid ECA, was designed to be coupled with methoxy polyethylene glycol-polylactide MPEG–PLA by disulfide bonds to prepare methoxy polyethylene glycol-polylactide-disulphide bond-mthacrynic acid MPEG–PLA–SS–ECA as a carrier material of the nanoparticles. Nanoparticles of pingyangmycin PYM and carboplatin CBP were prepared, respectively, and their physicochemical properties were investigated. The ECA at the disulfide could be released in the presence of GSH, the pingyangmycin, carboplatin and ECA were all uniformly released, and the nanoparticles could release all the drugs completely within 10 days. The half maximal inhibitory concentration IC50 of the prepared MPEG–PLA–SS–ECA-CBP and MPEG–PLA–SS–ECA-PYM nanoparticles in drug-resistant oral squamous cell carcinoma cell lines SCC15-CBP and SCC15-PYM cells was 12.68 μg·mL−1 and 12.76 μg·mL−1, respectively; the resistant factor RF of them in the drug-resistant cells were 1.51 and 1.24, respectively, indicating that MPEG–PLA–SS–ECA nanoparticles can reverse the drug resistance of these two drug-resistant cells. View Full-Text

Keywords: nanoparticle; GST inhibitor; redox-sensitive; self-assembly nanoparticle; GST inhibitor; redox-sensitive; self-assembly





Autor: Bing Han 1, Yanli Wang 2, Lan Wang 3, Zuhui Shang 3, Shuang Wang 4 and Jin Pei 1,*

Fuente: http://mdpi.com/



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