a Department of Oncology , The Second Affiliated Hospital of Soochow University, Institute of Radiotherapy & Oncology, Soochow University , Suzhou , China.
b Department of Plastic Surgery , The Second Affiliated Hospital of Soochow University , Suzhou , China.
Artif Cells Nanomed Biotechnol. 2018 Dec;46(8):1864-1871. doi: 10.1080/21691401.2017.1394874. Epub 2017 Oct 30.
The aim of the present study was to prepare a novel CD133 aptamer modified DTX liposome system and investigate its characteristics in vitro and in vivo studies. In this study, the CD133-DTX LP was prepared by the thin-film hydration method and with the particle size of 100-120 nm. The TEM photomicrographs were smooth, sub-spherical in shape and aggregated to form small clusters. In vitro, a relatively slower DTX release profile was observed in CD133-DTX LP due to the presence of CD133 aptamers on the outer surface which might hinder the drug release. The drug release mechanism fit well with the Higuchi equation better. In cytotoxicity study, CD133 aptamers modified DTX LP significantly decreased cell proliferation and improved the therapeutic efficiency. In vivo imaging result indicated that CD133-DTX LP had very good tumour targeting ability. In vivo antitumour activity indicated that the CD133-DTX LP showed a significant antitumour activity in A549 tumour mice, with a very low systemic toxicity.
本研究旨在制备一种新型的 CD133 适体修饰的多柔比星脂质体系统，并对其进行体外和体内研究。在本研究中，采用薄膜水化法制备 CD133-DTX LP，粒径为 100-120nm。TEM 照片显示，其形状为光滑的亚球形，并聚集形成小簇。体外研究结果表明，由于 CD133 适体存在于脂质体的外表面，可能会阻碍药物的释放，因此 CD133-DTX LP 呈现出相对较慢的多柔比星释放曲线。药物释放机制更符合 Higuchi 方程。在细胞毒性研究中，CD133 适体修饰的多柔比星脂质体显著降低了细胞增殖，并提高了治疗效率。体内成像结果表明，CD133-DTX LP 具有很好的肿瘤靶向能力。体内抗肿瘤活性研究表明，CD133-DTX LP 在 A549 肿瘤小鼠中表现出显著的抗肿瘤活性，且全身毒性很低。
