bm9b01742_si_001.pdf (809.11 kB)
Enhancement of Loading Efficiency by Coloading of Doxorubicin and Quercetin in Thermoresponsive Polymeric Micelles
journal contribution
posted on 2020-03-13, 16:08 authored by Pooneh Soltantabar, Erika L. Calubaquib, Ebrahim Mostafavi, Michael C. Biewer, Mihaela C. StefanChemotherapy
faces challenges, including poor aqueous solubility
of the drugs, and cardiotoxicity. Micellar drug delivery systems (DDS)
are used to encapsulate anticancer drugs for better therapeutic effects,
however, with poor loading content. Herein, we synthesized a micellar
DDS using γ-benzyloxy substituted poly(ε-caprolactone)
as the hydrophobic block and coloaded anticancer doxorubicin (Dox)
and antioxidant quercetin (Que). γ-Substituted oligo(ethylene)
glycol (OEG) poly(ε-caprolactone)s were used as hydrophilic
blocks to make the polymers thermoresponsive. Variation of the OEG
chain allowed the tunability of the lower critical solution temperature.
Moreover, drug loading and release were studied. Thermodynamic stability,
size, and morphology were determined by fluorescence measurements,
dynamic light scattering, and transmission electron microscopy. Combination
loading demonstrated improved loading of Dox and Que. Biological studies
were performed using HepG2 human liver cancer and H9c2 rat heart cells.
The use of biodegradable, biocompatible, and thermoresponsive polymers
along with the coloading approach is a good strategy in developing
DDSs.
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Keywords
Thermodynamic stabilityCombination loadingantioxidant quercetincoloading approachthermoresponsive polymersMicellar drug delivery systemsBiological studiesmicellar DDSQueliver cancerLoading EfficiencyH 9c rat heart cellsanticancer drugsγ- benzyloxysolution temperaturetransmission electron microscopyOEG chainpolymers thermoresponsiveThermoresponsive Polymeric Micelles Chemotherapycoloaded anticancer doxorubicindrug loadingfluorescence measurementsDoxloading contentHepG 2
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