软骨细胞亲和肽修饰的 PAMAM 缀合物作为一种纳米平台，用于靶向和在软骨中保留。
Chondrocyte affinity peptide modified PAMAM conjugate as a nanoplatform for targeting and retention in cartilage.
机构信息
Department of Pharmaceutics, College of Pharmaceutical Sciences, Soochow University, Suzhou 215123, PR China.
Department of Pharmaceutics, College of Pharmaceutical Sciences, Fujian Medical University, Fuzhou 350108, PR China.
出版信息
Nanomedicine (Lond). 2018 Apr 1;13(7):749-767. doi: 10.2217/nnm-2017-0335. Epub 2018 Mar 12.
AIM
To develop a nanocarrier for targeted delivery of agents to the cartilage.
MATERIALS & METHODS: Chondrocyte affinity peptide modified PEGylated polyamidoamine conjugates (CAP-PEG-PAMAM) were prepared and rhodamine B isothiocyanate (RB) fluorophore was linked on them for comparative biological tracing and profiling.
RESULTS
CAP4-PP-RB exhibited much more efficient cellular uptake in vitro than that of PEG-PAMAM-RB. Both the conjugates were likely internalized by chondrocytes via clathrin and caveolin co-mediated endocytosis, and delivered to lysosomes. In vivo imaging demonstrated the fluorescein-labeled nanocarrier was capable to persist in the joint cavity of rats for a prolonged time. Furthermore, the CAP4-PEG-PAMAM showed a good biocompatibility and enhanced penetration effects in vivo.
CONCLUSION
CAP-PEG-PAMAM could be an effective nanocarrier for intra-articular delivery of agents to cartilage.
目的
开发一种用于将药物靶向递送至软骨的纳米载体。
材料与方法
制备了软骨细胞亲和肽修饰的聚乙二醇化聚酰胺胺缀合物（CAP-PEG-PAMAM），并将罗丹明 B 异硫氰酸酯（RB）荧光染料连接在其上，用于比较生物示踪和分析。
结果
CAP4-PP-RB 在体外的细胞摄取效率明显高于 PEG-PAMAM-RB。两种缀合物都可能通过网格蛋白和小窝蛋白共介导的内吞作用被软骨细胞内化，并被递送至溶酶体。体内成像表明，荧光素标记的纳米载体能够在大鼠关节腔内长时间存在。此外，CAP4-PEG-PAMAM 表现出良好的生物相容性和体内增强渗透作用。
结论
CAP-PEG-PAMAM 可作为一种有效的关节内递药纳米载体，用于向软骨输送药物。
Zotero 插件