载顺铂的聚丙烯酸-甲基丙烯酸甲酯共聚物纳米粒子。
Cisplatin-incorporated nanoparticles of poly(acrylic acid-co-methyl methacrylate) copolymer.
机构信息
Department of Oriental Medicine Materials, Dongshin University, Naju, South Korea.
出版信息
Int J Nanomedicine. 2013;8:2835-45. doi: 10.2147/IJN.S48367. Epub 2013 Aug 8.
BACKGROUND
Although cisplatin is extensively used in the clinical field, its intrinsic toxicity limits its clinical use. We investigated nanoparticle formations of poly(acrylic acid-co-methyl methacrylate) (PAA-MMA) incorporating cisplatin and their antitumor activity in vitro and in vivo.
METHODS
Cisplatin-incorporated nanoparticles were prepared through the ion-complex formation between acrylic acid and cisplatin. The anticancer activity of cisplatin-incorporated nanoparticles was assessed with CT26 colorectal carcinoma cells.
RESULTS
Cisplatin-incorporated nanoparticles have small particle sizes of less than 200 nm with spherical shapes. Drug content was increased according to the increase of the feeding amount of cisplatin and acrylic acid content in the copolymer. The higher acrylic acid content in the copolymer induced increase of particle size and decrease of zeta potential. Cisplatin-incorporated nanoparticles showed a similar growth-inhibitory effect against CT26 tumor cells in vitro. However, cisplatin-incorporated nanoparticles showed improved antitumor activity against an animal tumor xenograft model.
CONCLUSION
We suggest that PAA-MMA nanoparticles incorporating cisplatin are promising carriers for an antitumor drug-delivery system.
背景
顺铂在临床领域被广泛应用，但由于其固有毒性限制了其临床应用。我们研究了聚（丙烯酸-co-甲基丙烯酸甲酯）（PAA-MMA）结合顺铂形成的纳米颗粒及其在体外和体内的抗肿瘤活性。
方法
通过丙烯酸和顺铂之间的离子络合形成顺铂结合纳米颗粒。用 CT26 结直肠癌细胞评估顺铂结合纳米颗粒的抗癌活性。
结果
顺铂结合纳米颗粒的粒径小于 200nm，呈球形。药物含量随着顺铂和共聚物中丙烯酸含量的增加而增加。共聚物中较高的丙烯酸含量会导致粒径增大和zeta 电位降低。顺铂结合纳米颗粒对 CT26 肿瘤细胞在体外表现出相似的生长抑制作用。然而，顺铂结合纳米颗粒对动物肿瘤异种移植模型表现出改善的抗肿瘤活性。
结论
我们认为，结合顺铂的 PAA-MMA 纳米颗粒是一种有前途的抗肿瘤药物传递系统载体。
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