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用于靶向递送抗癌药物的磁性微胶囊。

Magnetic microcapsules for targeted delivery of anticancer drugs.

作者信息

Kato T, Nemoto R, Mori H, Abe R, Unno K, Goto A, Murota H, Harada M, Homma M

出版信息

Appl Biochem Biotechnol. 1984;10:199-211. doi: 10.1007/BF02783752.

Abstract

To achieve targeted distribution of anticancer drugs with sustained activity, ferromagnetic ethylcellulose microcapsules containing an anticancer drug, mitomycin C (FM-MMC-mc), were prepared by a method based on phase separation principles. Two prototypes of FM-MMC-mc were made: one with the drug as the core and zinc ferrite on its capsular surface (outer type); the other with both the drug and zinc ferrite as the core (inner type). Both preparations provided a sustained-release property and a sensitive response to conventional magnetic force, although certain differences in the release rate of drug, magnetic responsiveness, and particle size were found between the two dosage forms. Animal studies showed that the magnetic microcapsules could be magnetically controlled in the artery and urinary bladder. VX2 tumors in the rabbit hind limb and urinary bladder were successfully treated with magnetic control of FM-MMC-mc. Pharmacokinetic study revealed that the targeting of the microcapsules markedly enhanced the drug absorption into the surrounding tissues for a prolonged period of time. The results indicate the feasibility and effectiveness of the magnetic microcapsules as a targeted drug delivery system.

摘要

为实现具有持续活性的抗癌药物的靶向分布,基于相分离原理,制备了含有抗癌药物丝裂霉素C的铁磁性乙基纤维素微胶囊(FM-MMC-mc)。制备了两种FM-MMC-mc原型:一种是以药物为核心,在其囊膜表面包裹铁酸锌(外剂型);另一种是以药物和铁酸锌均为核心(内剂型)。两种制剂均具有缓释特性且对传统磁力有灵敏响应,尽管两种剂型在药物释放速率、磁响应性和粒径方面存在一定差异。动物研究表明,磁性微胶囊可在动脉和膀胱中通过磁力控制。通过对FM-MMC-mc进行磁力控制,成功治疗了兔后肢和膀胱中的VX2肿瘤。药代动力学研究表明,微胶囊的靶向性显著增强了药物在较长时间内对周围组织的吸收。结果表明磁性微胶囊作为靶向给药系统具有可行性和有效性。

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