小粒径氟尿嘧啶隐形泡囊的制备、表征及其抗癌作用评价

发布时间：2018-08-12 13:14

【摘要】：目的:制备小粒径氟尿嘧啶隐形泡囊给药系统,对其进行理化表征并研究其体内外抗癌作用。方法:采用溶剂注入法制备泡囊,经过形态、粒径、包封率和体外释放规律等物理性质考察,并通过对2种癌细胞的细胞毒性实验及对balb/c荷瘤鼠抑瘤实验评价其抗癌作用。结果:制得的泡囊为球形、平均粒径240.4 nm、Zeta电位为-68.37 m V、表面水化层厚度1.83 nm、包封率32.76%;泡囊的体外释放符合Weibull模型,在模拟正常体液中释药减缓(t1/2为游离氟尿嘧啶的3.47倍)。泡囊在体外对癌细胞的生长抑制作用显著,对细胞的IC_(50)降低为游离Fu的9.1%~18.4%(P0.01)。泡囊对balb/c荷瘤鼠的瘤增长抑制明显,抑瘤率由同浓度游离药物的19.58%增加至48.45%。结论:本实验制备的小粒径氟尿嘧啶泡囊性能好,缓释性能明显,细胞实验、动物实验均表明抗癌作用显著,是一种具有良好开发前景的新型微粒给药系统。
[Abstract]:Aim: to prepare a drug delivery system with small particle size fluorouracil (FU) invisible vesicle, and to characterize the drug delivery system and to study its anticancer effect in vivo and in vitro. Methods: the vesicle was prepared by solvent injection method. The morphology, particle size, encapsulation efficiency and release rule in vitro were investigated. The anticancer effects of the two kinds of cancer cells were evaluated by the cytotoxicity test and the tumor inhibition test on balb/c tumor-bearing mice. Results: the vesicle was spherical, the average particle size was -68.37 MV, the thickness of surface hydration layer was 1.83 nm, the encapsulation efficiency was 32.76.The release of vesicle in vitro was consistent with Weibull model, and the release of drug in simulated normal body fluid was slowed down (t 1 / 2 was 3.47 times of free fluorouracil). The inhibitory effect of vesicle on the growth of cancer cells was significant in vitro, and the IC50 of the cells was reduced to 9.1g / L of free Fu (P0.01). The vesicular sac inhibited the tumor growth of balb/c bearing mice obviously, and the inhibition rate increased from 19.58% of the same concentration of free drugs to 48.45%. Conclusion: the small diameter fluorouracil vesicles prepared in this experiment have good performance and obvious sustained release. The cell experiments and animal experiments show that the anti-cancer effect is remarkable and it is a new drug delivery system with good development prospect.
【作者单位】：苏州大学药学院;
【基金】：国家自然科学基金(81473166)
【分类号】：R943;R96

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