Pharmacokinetics and antitumor efficacy of DSPE-PEG2000 polymeric liposomes loaded with quercetin and temozolomide: Analysis of their effectiveness in enhancing the chemosensitization of drug-resistant glioma cells

International Journal of Molecular Medicine
Jun HuXiaoqian Dang

Abstract

In the present study, a new type of DSPE-PEG2000 polymeric liposome for the brain-targeted delivery of poorly water-soluble anticancer drugs was successfully prepared and characterized. The nanoparticles were formed by the self-assembly of an amphiphilic polymer consisting of hydrophilic 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000] (DSPE‑PEG2000). These nanoliposomes served as a safe delivery platform for the simultaneous delivery of quercetin (QUE) and temozolomide (TMZ) to rat brains. The 2-in-1 PEG2000‑DSPE nanoliposomes containing QUE and TMZ (QUE/TMZ-NLs) were rapidly taken up by the U87 glioma cells in vitro, whereas at the same concentrations, the amounts of the free drugs taken up were minimal. The QUE/TMZ-NLs showed an enhanced potency in the U87 cells and the TMZ-resistant U87 cells (U87/TR cells), possibly due to the high intracellular drug concentration and the subsequent drug release. In vivo biodistribution experiments revealed a significant accumulation of QUE/TMZ-NLs in the brain, with significantly increased plasma concentrations of QUE and TMZ, as well as delayed clearance in our rat model of glioma. The results were not so significant for the QUE-loaded nanoliposomes (...Continue Reading

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Citations

Feb 13, 2019·Reviews in the Neurosciences·Elnaz AmanzadehMaryam Nourbakhshnia
Sep 20, 2018·Current Drug Delivery·Tapan Kumar Giri
Dec 5, 2019·Anais Da Academia Brasileira De Ciências·Juliana M SoaresLuciana F Romão
Oct 24, 2018·International Journal of Molecular Sciences·Sangiliyandi GurunathanJin-Hoi Kim
Jul 10, 2019·Anti-cancer Agents in Medicinal Chemistry·Manjula Vinayak, Akhilendra K Maurya
Jul 4, 2021·Colloids and Surfaces. B, Biointerfaces·Güliz AkŞenay Hamarat Şanlıer

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Methods Mentioned

BETA
electrophoresis
infrared spectroscopy
fluorescence microscopy
enzyme-linked immunosorbent assay

Software Mentioned

FV10
ASW
Statistical Program for Social Sciences ( SPSS )
SPSS

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