新型改性壳聚糖靶向抗肿瘤药物传递的体外评价。
In vitro evaluation on novel modified chitosan for targeted antitumor drug delivery.
机构信息
Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, PR China.
出版信息
Carbohydr Polym. 2013 Jan 30;92(1):545-54. doi: 10.1016/j.carbpol.2012.08.112. Epub 2012 Sep 6.
In this study, a novel amphiphilic copolymer designed as N-octyl-N-phthalyl-3,6-O-(2-hydroxypropyl) chitosan (OPHPC) were synthesized and then conjugated with folic acid (FA-OPHPC) to produce a targeted drug carrier for tumor-specific drug delivery. OPHPC and FA-OPHPC were characterized by FT-IR, (1)H NMR, (13)C NMR and elemental analysis. Paclitaxel (PTX) loaded OPHPC micelles (PTX-OPHPC) with well-defined spherical shape and homogeneous distribution exhibited drug-loading rate ranging from 33.6% to 45.3% and entrapment efficiency from 50.5% to 82.8%. In the cellular uptake studies, PTX-OPHPC brought about a significantly higher amount of PTX accumulated in human breast adenocarcinoma cell line (MCF-7 cells) compared with Taxol. Moreover, the cellular uptake of PTX in PTX loaded FA-OPHPC micelles (PTX-FA-OPHPC) was 3.2-fold improved in comparison with that of PTX-OPHPC. The results revealed that OPHPC micelle might be a promising drug carrier for promoting PTX cellular uptake and FA-OPHPC micelle could be used as a potential tumor-targeted drug vector.
在这项研究中，设计了一种新型两亲性共聚物 N-辛基-N-邻苯二甲酰基-3,6-O-(2-羟丙基)壳聚糖（OPHPC），然后将其与叶酸（FA-OPHPC）缀合，以产生用于肿瘤特异性药物递送的靶向药物载体。通过傅里叶变换红外光谱（FT-IR）、（1）H NMR、（13）C NMR 和元素分析对 OPHPC 和 FA-OPHPC 进行了表征。具有明确的球形形状和均匀分布的紫杉醇（PTX）负载的 OPHPC 胶束（PTX-OPHPC）的载药率范围为 33.6%至 45.3%，包封效率为 50.5%至 82.8%。在细胞摄取研究中，与 Taxol 相比，PTX-OPHPC 使更多的 PTX 积聚在人乳腺癌腺癌细胞系（MCF-7 细胞）中。此外，与 PTX-OPHPC 相比，负载 PTX 的 FA-OPHPC 胶束（PTX-FA-OPHPC）中的 PTX 细胞摄取增加了 3.2 倍。结果表明，OPHPC 胶束可能是促进 PTX 细胞摄取的有前途的药物载体，FA-OPHPC 胶束可用作潜在的肿瘤靶向药物载体。
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