Development polymeric micellar system for targeted delivery of antitumor drugs

Kunitskaya, L. R.; Zheltonozhskaya, Tatyana; Gerda, V. I.; Klepko, V.V.

doi:10.1007/s13204-021-01876-7

Cited by 3 publications

(1 citation statement)

References 21 publications

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“…Many articles have reported that attaching PEG to molecules or nanoparticles decreases their clearance rate from the body because PEG polymers can protect them from the recognition and phagocytosis by the reticuloendothelial system (RES) and prolong their half-life in the bloodstream ( Babu et al, 2014 ; Rastogi et al, 2020 ; Rommasi and Esfandiari, 2021 ; Cheng et al, 2021 ; Kunitskaya et al, 2021 ).…”

Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of the Cytoprotective Activity of Micelles with DSPE-PEG-C60 as a Carrier Against Doxorubicin-Induced Cytotoxicity

Ding

et al. 2022

Front. Pharmacol.

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To deliver doxorubicin (DOX) with enhanced efficacy and safety in vivo, fullerenol-modified micelles were prepared with the amphiphilic polymer DSPE-PEG-C60 as a carrier, which was synthesized by linking C60(OH)22 with DSPE-PEG-NH2. Studies of its particle size, PDI, zeta potential, and encapsulation efficiency were performed. DOX was successfully loaded into the micelles, exhibiting a suitable particle size [97 nm, 211 nm, 260 nm, vector: DOX = 5:1, 10:1; 15:1 (W/W)], a negative zeta potential of around −30 mv, and an acceptable encapsulation efficiency [86.1, 95.4, 97.5%, vector: DOX = 5:1, 10:1; 15:1 (W/W)]. The release behaviors of DOX from DSPE-PEG-C60 micelles were consistent with the DSPE-PEG micelles, and it showed sustained release. There was lower cytotoxicity of DSPE-PEG-C60 micelles on normal cell lines (L02, H9c2, GES-1) than free DOX and DSPE-PEG micelles. We explored the protective role of DSPE-PEG-C60 on doxorubicin-induced cardiomyocyte damage in H9c2 cells, which were evaluated with a reactive oxygen species (ROS) assay kit, JC-1, and an FITC annexin V apoptosis detection kit for cellular oxidative stress, mitochondrial membrane potential, and apoptosis. The results showed that H9c2 cells exposed to DSPE-PEG-C60 micelles displayed decreased intracellular ROS, an increased ratio of red fluorescence (JC-1 aggregates) to green fluorescence (JC-1 monomers), and a lower apoptotic ratio than the control and DSPE-PEG micelle cells. In conclusion, the prepared DOX-loaded DSPE-PEG-C60 micelles have great promise for safe, effective tumor therapy.

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