Zhou Lin, Huang Zhi, Yang Shanyi, Wei Jiarui, Xu Yan, Hu Lin, Guo Xinrong, Yuan Limin, Yuan Zexuan, Yang Xiaoping, Tao Xiaojun, Zhang Qiufang
Department of Geriatrics and General Medicine (QZ) of Affiliated Taihe Hospital, Pharmaology Department (LZ, JW, XG, QZ), School of Basic Medical Science, Hubei University of Medicine, Shiyan, 442000, Hubei, China.
Key Laboratory of Study and Discovery of Small Targeted Molecules of Hunan Province (ZH, SY, YX, LY, ZY, XY, XT), School of Medicine, Hunan Normal University, Changsha, China.
Nanoscale Res Lett. 2021 Oct 17;16(1):155. doi: 10.1186/s11671-021-03609-9.
Hydrophilic polyethylene glycol monomethyl ether (mPEG) was grafted onto Icariin (ICA) by succinic anhydride to form a polyethylene glycol-Icariin (mPEG-ICA) polymer. The structure of the polymer was characterized by Fourier transform infrared spectroscopy (FT-IR) and nuclear magnetic resonance spectroscopy (NMR). mPEG-ICA nanoparticles loaded with ICA were prepared by physical embedding of ICA by dialysis. The particle size was determined to be (220 ± 13.7) nm, and the ζ potential was (2.30 ± 1.33) mV by dynamic light scattering (DLS). Under a transmission electron microscope (TEM), the nanoparticles were spherical, and the morphology was regular. In the medium with pH 7.4, the drug release rate of mPEG-ICA nanoparticles reached (52.80 ± 1.70)% within 72 h. At pH 6.8, the cumulative drug release of nanoparticles reached (75.66 ± 0.17)% within 48 h. Treatment of the nanoparticles with LPS-treated H9c2 cells maintained cell viability, reduced LDH release and exerted antiapoptotic effects. Moreover, ICA-loaded mPEG-ICA nanoparticles significantly decreased the mRNA expression of the myocardial inflammatory cytokines TNF-α, IL-1β and IL-6M. In conclusion, ICA-loaded mPEG-ICA nanoparticles protected against LPS-induced H9c2 cell injury.
通过琥珀酸酐将亲水性聚乙二醇单甲醚（mPEG）接枝到淫羊藿苷（ICA）上，形成聚乙二醇 - 淫羊藿苷（mPEG - ICA）聚合物。通过傅里叶变换红外光谱（FT - IR）和核磁共振光谱（NMR）对聚合物结构进行表征。通过透析物理包埋ICA制备负载ICA的mPEG - ICA纳米颗粒。通过动态光散射（DLS）测定粒径为（220±13.7）nm，ζ电位为（2.30±1.33）mV。在透射电子显微镜（TEM）下，纳米颗粒呈球形，形态规则。在pH 7.4的介质中，mPEG - ICA纳米颗粒的药物释放率在72小时内达到（52.80±1.70）%。在pH 6.8时，纳米颗粒的累积药物释放在48小时内达到（75.66±0.17）%。用LPS处理的H9c2细胞处理纳米颗粒可维持细胞活力，减少乳酸脱氢酶（LDH）释放并发挥抗凋亡作用。此外，负载ICA的mPEG - ICA纳米颗粒显著降低心肌炎性细胞因子TNF - α、IL - 1β和IL - 6M的mRNA表达。总之，负载ICA的mPEG - ICA纳米颗粒可保护细胞免受LPS诱导的H9c2细胞损伤。
