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Enhancement of Loading Efficiency by Coloading of Doxorubicin and Quercetin in Thermoresponsive Polymeric Micelles.
Biomacromolecules ( IF 6.2 ) Pub Date : 2020-03-09 , DOI: 10.1021/acs.biomac.9b01742
Pooneh Soltantabar , Erika L Calubaquib , Ebrahim Mostafavi 1 , Michael C Biewer , Mihaela C Stefan
Affiliation  

Chemotherapy 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.

中文翻译:

通过在热响应性聚合物胶束中共同装载阿霉素和槲皮素来提高装载效率。

化学疗法面临挑战,包括药物的水溶性差和心脏毒性。胶束药物递送系统(DDS)用于封装抗癌药物,以获得更好的治疗效果,但是负载量较弱。在这里,我们合成了胶束DDS,使用γ-苄氧基取代的聚(ε-己内酯)作为疏水性嵌段,并负载抗癌阿霉素(Dox)和抗氧化剂槲皮素(Que)。γ取代的低聚乙二醇(OEG)聚(ε-己内酯)被用作亲水性嵌段,以使聚合物具有热响应性。OEG链的变化允许较低临界溶液温度的可调性。此外,还研究了药物的负载和释放。热力学稳定性,大小和形态通过荧光测量,动态光散射,和透射电子显微镜。组合载荷表明Dox和Que的载荷得到了改善。使用HepG2人肝癌和H9c2大鼠心脏细胞进行了生物学研究。在开发DDS时,使用可生物降解,生物相容性和热响应性聚合物以及共载方法是一种很好的策略。
更新日期:2020-04-23
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