Biological and Chemical Engineering College, Anhui Polytechnic University, Beijing Middle Road, Anhui, 241000, Wuhu, China.
Department of Microbiology and immunology, Wannan Medical College, No. 22 Wenchang West Road, 241002, Wuhu, China.
J Mater Sci Mater Med. 2018 Dec 19;30(1):3. doi: 10.1007/s10856-018-6204-8.
A new tumor-targeted drug-loading material, the amphiphilic peptide DGRGGGAAAA (P10) was designed and synthesized, and its self-assembly behavior, drug-loading effects and in vitro characteristics were studied. P10 was synthesized by solid-state synthesis and doxorubicin (DOX) was loaded via dialysis. P10 and DOX were mixed with a mass ratio of 6:1 to form regular round spheres. The interconnection between groups was analyzed spectroscopically and the sphere morphology was studied with SEM and a zeta particle size analyzer. Fluorescence spectroscopy was used to analyze the ability of P10 to form micelles and the efficiency of micelle entrapment, and the drug-loading ratio and drug release characteristics were detected. Finally, the in vitro antitumor activity of P10 was studied with HeLa cells as a model. The results showed that P10's critical micelle concentration (CMC) value and its average grain diameter were approximately 0.045 mg/L and 500 nm. The micelle entrapment ratio and drug-loading ratio were 23.011 ± 2.88 and 10.125 ± 2.62%, respectively, and the in vitro drug-releasing properties of P10 were described by the Zero-order model and the Ritger-Peppas model. Compared with DOX, P10-DOX had a higher tumor cell inhibition ratio and a dose-effect relationship with concentration. When P10-DOX's concentration was 20 μg/mL, the inhibition ratio was 44.17%. The new amphiphilic peptide designed and prepared in this study could be a tumor-targeted drug-loading material with better prospects for application. In this paper, a new tumor-targeted drug-loading material, the amphiphilic peptide DGRGGGAAAA (P10) is designed and synthesized, and its self-assembly behavior, drug-loading effects and in vitro characteristics are studied, providing a theoretical basis and design ideas for further studies and the development of targeted drug-loading materials on tumor cells.
一种新的肿瘤靶向药物载体制备材料，两亲性肽 DGRGGGAAAA（P10）被设计并合成，并研究了其自组装行为、载药效果和体外特性。P10 通过固相合成法合成，阿霉素（DOX）通过透析法负载。P10 和 DOX 以质量比 6:1 混合形成规则的圆形球体。通过光谱分析基团之间的连接，并通过 SEM 和 Zeta 粒径分析仪研究球体形态。荧光光谱法用于分析 P10 形成胶束的能力和胶束包封效率，并检测载药率和药物释放特性。最后，以 HeLa 细胞为模型研究 P10 的体外抗肿瘤活性。结果表明，P10 的临界胶束浓度（CMC）值及其平均粒径约为 0.045mg/L 和 500nm。胶束包封率和载药率分别为 23.011±2.88%和 10.125±2.62%，P10 的体外药物释放特性符合零级模型和 Ritger-Peppas 模型。与 DOX 相比，P10-DOX 对肿瘤细胞的抑制率更高，且具有浓度依赖性。当 P10-DOX 的浓度为 20μg/mL 时，抑制率为 44.17%。本研究设计和制备的新型两亲性肽可能是一种具有良好应用前景的肿瘤靶向药物载体制备材料。本文设计并合成了一种新的肿瘤靶向药物载体制备材料，两亲性肽 DGRGGGAAAA（P10），并研究了其自组装行为、载药效果和体外特性，为进一步研究和开发针对肿瘤细胞的靶向药物载体制备材料提供了理论依据和设计思路。
