<p>Combined Delivery of Temozolomide and siPLK1 Using Targeted Nanoparticles to Enhance Temozolomide Sensitivity in Glioma</p>

• DOI: 10.2147/ijn.s243878
• Publication Date: 2020-05-11T23:44:31Z
• Authors: Hui Shi; Shuo Sun; Haoyue Xu; Zongren Zhao; Zhengzhong Han; Jun Jia; Dongmei Wu; Jun Lu; Hongmei Liu; Rutong Yu
• Keywords: Temozolomide

Introduction: Temozolomide (TMZ) is the first-line chemotherapeutic option to treat glioma; however, its efficacy and clinical application are limited by drug resistance properties. Polo-like kinase 1 (PLK1)-targeted therapy causes G2/M arrest increases sensitivity of glioma TMZ. Therefore, limit TMZ in glioma, an angiopep-2 (A2)-modified polymeric micelle (A2PEC) embedded with a small interfering RNA (siRNA) targeting PLK1 (siPLK1) was developed (TMZ-A2PEC/siPLK). Materials Methods: encapsulated A2-PEG-PEI-PCL through hydrophobic interaction, siPLK1 complexed TMZ-A2PEC electrostatic interaction. Then, (A2) modified embedding siRNA polo-like Results: In vitro experiments indicated that TMZ-A2PEC/siPLK effectively enhanced cellular uptake resulted significant cell apoptosis cytotoxicity cells. vivo showed growth inhibited, survival time animals prolonged remarkably after TMZ-A2PEC/siPLK1 injected via their tail vein. Discussion: The results demonstrate combination A2PEC could enhance treating glioma. Keywords: co-delivery, micelle, siPLK1, TMZ, resistance,