Department of Thoracic Surgery, Shanghai Shidong Hospital, Shanghai, 200438, People's Republic of China.
Drug Des Devel Ther. 2022 Jun 8;16:1767-1778. doi: 10.2147/DDDT.S366531. eCollection 2022.
Mangiferin is a plant antitumor compound with poor water solubility and low bioavailability. In this study, transferrin-modified mangiferin-loaded solid lipid nanoparticles (Tf-modified MGF-SLNs) were prepared to overcome the above defects.
Tf-modified MGF-SLNs were prepared by the emulsification-solvent evaporation method. The physicochemical properties of Tf-MGF-SLNs such as particle size, zeta potential and in vitro drug release were investigated. We also demonstrated the effect of Tf-MGF-SLNs in lung cancer.
The mean hydrodynamic diameter of the Tf-MGF-SLNs was 121.8±2.9 nm with a polydispersity index of 0.134±0.03. According to TEM micrographs, Tf-MGF-SLNs are spherical and uniform, and the EE% was found to be 72.5±2.4%. In vitro release, we identified an initial burst effect release, followed by controlled release, in SLNs at both pHs and the Tf-MGF-SLNs drug accumulation release percentages reached over 68% at pH 4.0 and 72% at pH 7.4 in 6 hours, respectively. In vivo studies showed that depending on surface modification, Tf-MGF-SLNs, which suggested that cell internalization was changed and more drugs entered the cells successfully.
Tf-MGF-SLNs were highly efficient in suppressing the tumor growth in xenograft tumor model. Sustained release of the drug delivery system and Tf-modified MGF-SLNs played a major role. Tf-MGF-SLNs would be a promising formulation for the treatment of lung cancer.
山竹堿是一种植物抗肿瘤化合物,具有较差的水溶性和较低的生物利用度。本研究制备了转铁蛋白修饰的山竹堿载固体脂质纳米粒(Tf-修饰的 MGF-SLNs)以克服上述缺陷。
采用乳化溶剂蒸发法制备 Tf-修饰的 MGF-SLNs。考察了 Tf-MGF-SLNs 的粒径、Zeta 电位和体外药物释放等理化性质,并研究了 Tf-MGF-SLNs 对肺癌的作用。
Tf-MGF-SLNs 的平均水动力直径为 121.8±2.9nm,多分散指数为 0.134±0.03。根据 TEM 显微照片,Tf-MGF-SLNs 呈球形且均匀,EE%为 72.5±2.4%。体外释放结果表明,在两种 pH 值下,SLNs 均表现出初始突释效应释放,随后为控制释放,Tf-MGF-SLNs 在 pH 4.0 时的药物累积释放百分比在 6 小时内超过 68%,在 pH 7.4 时超过 72%。体内研究表明,通过表面修饰,Tf-MGF-SLNs 可以改变细胞内化,使更多的药物成功进入细胞。
Tf-MGF-SLNs 能够高效抑制异种移植瘤模型中的肿瘤生长。药物传递系统的持续释放和 Tf 修饰的 MGF-SLNs 发挥了重要作用。Tf-MGF-SLNs 将成为治疗肺癌的一种有前途的制剂。