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磁性PECA纳米颗粒作为靶向给药的药物载体:合成与释放特性

Magnetic PECA nanoparticles as drug carriers for targeted delivery: synthesis and release characteristics.

作者信息

Yang J, Lee H, Hyung W, Park S-B, Haam S

机构信息

Department of Chemical Engineering, College of Engineering, Yonsei University, Seoul, South Korea.

出版信息

J Microencapsul. 2006 Mar;23(2):203-12. doi: 10.1080/02652040500435444.

DOI:10.1080/02652040500435444
PMID:16754376
Abstract

Magnetic poly(ethyl-2-cyanoacrylate) (PECA) nanoparticles containing anti-cancer drugs (Cisplatin and Gemcitabine) were prepared by inter-facial polymerization. The spherical nanoparticles (d = 250 +/- 15 nm) with smooth surfaces and moderately uniform size distributions were obtained. The amount of magnetite encapsulated inside the polymer matrix was increased up to 14.26% (w/w) by controlling the initial weight ratio of monomer/magnetite. It was found that the amount of Cisplatin encapsulated in the magnetic nanoparticle is much higher than that of Gemcitabine because Cisplatin (hydrophobic) is highly soluble in the oil phase and encapsulated easier inside nanoparticles compared to Gemcitabine (hydrophilic). The presence of magnetite and its super-paramagnetic characteristic were confirmed by FTIR spectra and VSM. In-vitro experiments of drug release and magnetic mobility under external magnetic field demonstrated that magnetic poly(ethyl-2-cyanoacrylate) (PECA) nanoparticles can be a highly versatile magnetic drug carrier with sustained release behaviour and sufficient magnetic susceptibility.

摘要

通过界面聚合法制备了负载抗癌药物(顺铂和吉西他滨)的磁性聚(乙基-2-氰基丙烯酸酯)(PECA)纳米颗粒。得到了表面光滑、尺寸分布适度均匀的球形纳米颗粒(直径d = 250±15 nm)。通过控制单体/磁铁矿的初始重量比,聚合物基质中封装的磁铁矿量增加到了14.26%(w/w)。研究发现,磁性纳米颗粒中封装的顺铂量远高于吉西他滨,这是因为顺铂(疏水性)在油相中高度可溶,与吉西他滨(亲水性)相比更容易封装在纳米颗粒内部。通过傅里叶变换红外光谱(FTIR)和振动样品磁强计(VSM)证实了磁铁矿的存在及其超顺磁性特征。体外药物释放和外磁场下磁迁移实验表明,磁性聚(乙基-2-氰基丙烯酸酯)(PECA)纳米颗粒可以成为一种具有缓释行为和足够磁化率的高度通用的磁性药物载体。

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