Biotinylated PAMAM dendrimers for intracellular delivery of cisplatin to ovarian cancer: role of SMVT.
Biotinylated PAMAM dendrimers for intracellular delivery of cisplatin to ovarian cancer: role of SMVT.
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发表时间：
2011-03
影响因子：
2
通讯作者：
V. Yellepeddi;Ajay Kumar;D. Maher;S. Chauhan;K. Vangara;S. Palakurthi
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作者：
V. Yellepeddi;Ajay Kumar;D. Maher;S. Chauhan;K. Vangara;S. Palakurthi
目的本研究的目的是制备负载顺铂的生物素化PAMAM树枝状大分子并评估其在卵巢癌细胞系中的细胞毒性。材料和方法 研究了生物素化和未缀合的树枝状大分子-顺铂复合物的包封效率、体外细胞毒性活性以及顺铂在 OVCAR-3、SKOV-3、A2780（野生型）和 CP70（A2780/CP70，顺铂耐药）细胞中的细胞积累。结果顺铂的包封率在5.33%~21.10%之间。体外细胞毒活性显示，在OVCAR-3、SKOV-3和CP70细胞系中，树枝状大分子-顺铂复合物的IC(50)值显着低于游离顺铂。细胞摄取数据显示，A2780 (19.41±0.85 μg/ml) 和 CP70 (25.25±1.25 μg/ml) 细胞系中顺铂的 PAMAMG(4) NH(2) 树枝状聚合物复合物对铂的积累最高，而 A2780 和 CP70 细胞系中的顺铂摄取仅为 1.77±0.351 μg/ml。 CP70 细胞中为 2.31±0.421 μg/ml。结论 总之，生物素化的 PAMAM 树枝状聚合物可用作顺铂递送至卵巢癌的潜在靶向剂。
AIM The aim of this study was to prepare biotinylated PAMAM dendrimers loaded with cisplatin and to evaluate the cytotoxicity in ovarian cancer cell lines. MATERIALS AND METHODS Biotinylated and unconjugated dendrimer-cisplatin complexes were investigated for encapsulation efficiency, in vitro cytotoxic activity and cellular accumulation of cisplatin in OVCAR-3, SKOV-3, A2780 (wild-type) and CP70 (A2780/CP70, cisplatin-resistant) cells. RESULTS Encapsulation efficiency of cisplatin ranged from 5.33% to 21.10%. In vitro cytotoxic activity revealed that IC(50) values of dendrimer-cisplatin complexes were significantly lower than that of free cisplatin in OVCAR-3, SKOV-3 and CP70 cell lines. Cellular uptake data showed highest accumulation of platinum by PAMAMG(4) NH(2) dendrimer complexes of cisplatin in A2780 (19.41±0.85 μg/ml) and CP70 (25.25±1.25 μg/ml) cell lines in comparison with cisplatin uptake of only 1.77±0.351 μg/ml in A2780 and 2.31±0.421 μg/ml in CP70 cells. CONCLUSION In conclusion, biotinylated PAMAM dendrimers may be utilized as potential targeting agents for cisplatin delivery to ovarian cancer.