四臂星形壳聚糖修饰的 PLGA 纳米粒作为新型载药平台用于伊立替康前药 SN38 的靶向递药
Tetrac-decorated chitosan-coated PLGA nanoparticles as a new platform for targeted delivery of SN38.
机构信息
a Pharmaceutical Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences , Mashhad , Iran.
b Department of Pharmaceutical Nanotechnology , School of Pharmacy, Mashhad University of Medical Sciences , Mashhad , Iran.
出版信息
Artif Cells Nanomed Biotechnol. 2018;46(sup2):1003-1014. doi: 10.1080/21691401.2018.1477789. Epub 2018 May 27.
New integrin-targeted nanoparticles made of chitosan-stabilized PLGA matrix was developed to specifically target colon adenocarcinoma. To this aim, SN38-encapsulated chitosan-coated PLGA NPs were conjugated with tetrac for integrin receptor-guided delivery. To provide a sustained release pattern for SN38, it was loaded into nanoparticles using single emulsion method. The size of NPs were 174.23 ± 6.12 nm with drug encapsulation efficiency and loading content of 73.16 ± 11.15 and 4.45 ± 0.31, respectively. The in vitro results confirmed that the designed nanoplatform showed specific cellular uptake and cytotoxicity in integrin overexpressing cancer cells and provided a sustained release profile for SN38. Additionally, an increased therapeutic potency of targeted formulation over both non-targeted and free drug was shown in vivo.
新型壳聚糖稳定的 PLGA 基质整合素靶向纳米颗粒被开发出来，以专门针对结肠腺癌。为此，将 SN38 包封的壳聚糖包覆的 PLGA NPs 与 tetrac 共轭，用于整合素受体引导的递药。为了提供 SN38 的持续释放模式，它被采用单相乳液法载入纳米颗粒中。NPs 的粒径为 174.23±6.12nm，药物包封效率和载药量分别为 73.16±11.15%和 4.45±0.31%。体外结果证实，所设计的纳米平台在整合素过表达的癌细胞中表现出特异性细胞摄取和细胞毒性，并为 SN38 提供了持续释放的特性。此外，体内研究表明，靶向制剂的治疗效果优于非靶向制剂和游离药物。
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