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目的制备负载冬凌草甲素(oridonin,ORI)的聚乙二醇功能化氧化石墨烯(PEGylated graphene oxide,GO-PEG)纳米粒(nanoparticles,NPs),并探讨其对结肠癌的抑制作用。方法利用酰胺化反应将端基为氨基的四臂聚乙二醇(PEG)连到氧化石墨烯(GO)上,并通过红外光谱(IR)和差示-热重联用热分析仪(TGA)等对其进行表征;再通过物理共混的方法在GO-PEG上负载抗肿瘤药物ORI,紫外光谱(UV)法测其包封率和载药率,MTT法测定载药体系对人结肠癌细胞SW620和HT29的增殖毒性,并建立荷瘤裸鼠模型考察其体内抗肿瘤活性。结果 IR和TGA测定结果表明PEG已成功偶联到GO上,UV法测得ORI-GO-PEG的包封率和载药率分别为95.81%和48.92%,且在各种生理溶液中具有良好的稳定性。体外细胞毒性实验结果表明,与ORI裸药相比,ORI-GO-PEG-NPs对结肠癌细胞的杀伤能力更强。体内抑瘤实验进一步发现,ORI-GO-PEG-NPs可以更好地抑制体内SW620肿瘤的生长。结论制得的ORI-GO-PEG-NPs具有优良的载药性能和较强的抗结肠癌作用,为今后开发抗肿瘤药物纳米给药系统提供了实验依据。
Objective To prepare PEGylated graphene oxide (GO-PEG) nanoparticles (or NPs) loaded with oridonin (ORI) and investigate its inhibitory effect on colon cancer. Methods Four-arm polyethylene glycol (PEG) with amino groups at the ends was connected to graphene oxide (GO) by amidation reaction and characterized by infrared spectroscopy (IR) and differential thermal- ) Were used to characterize the antitumor drug ORI on GO-PEG by physical blending. The entrapment efficiency and drug loading rate were measured by ultraviolet (UV) The proliferation of cancer cells SW620 and HT29 were studied. The tumor-bearing nude mice model was established to investigate the anti-tumor activity in vivo. Results The results of IR and TGA indicated that PEG was successfully coupled to GO. The entrapment efficiency and drug loading rate of ORI-GO-PEG measured by UV method were 95.81% and 48.92%, respectively, and were good in various physiological solutions Stability. In vitro cytotoxicity experiments showed that ORI-GO-PEG-NPs were more potent against colon cancer cells than ORIs. In vivo antitumor experiments further found that ORI-GO-PEG-NPs can better inhibit the growth of SW620 tumors in vivo. CONCLUSION: ORI-GO-PEG-NPs obtained in this study have excellent drug-loading properties and strong anti-colon cancer effect, which provides an experimental basis for the future development of anti-tumor drug nano-drug delivery system.