顺铂泡囊的研制与抗癌活性研究

Preparation of cis-diamminedichloroplatinum niosomes and its in vivo anti-tumor activity

目的:制备顺铂泡囊并对其进行理化性质和抗癌活性评价。方法:以Span40和胆固醇为主要材料制备泡囊,对其表面形态、粒径分布、电位、包封率、载药量及体外释放特性等理化性质进行考察,动物实验研究泡囊对荷VX2肉体瘤实验兔的体重变化、存活率、肿瘤生长和肿瘤细胞转移。结果:呈圆球状的泡囊粒径为(7.33±1.05)μm,包封率为(86.06±1.46)%,载药量为(3.04±0.05)%,体外释放实验t1/2在8 h附近。较之于市售制剂,存活率大大提高,毒性明显较小,更在抑制肿瘤生长和防止肿瘤细胞转移方面优势非常明显。结论:本实验研制的泡囊具有缓释作用和治疗肿瘤的高效低毒特点。

Objective： To prepare and characterize cis-diamminedichloroplatinum （CDDP） niosomes in vitro, and to evaluate their anti-tumor activity in vivo. Methods： The noisomes were prepared using Span40 and cholesterol as the main materials. Their morphology, particle size and distribution, electric potential, entrapment rate, drug-loading rate and release behavior in vitro were determined. Rabbits bearing VX2 sarcous tumor were sub- jected to anti-tumor tests, and the change in body weight, fraction surviving, tumor growth and cell metastasis were observed. Results ： The diameter of the round-looking niosomes was （7.33 ± 1.05） μm. The entrapment rate was （86.06±1.46）%, and drug loading rate was （3.04 ±0.05）%. In vitro release tests gave a t1/2 of about 8 h. Compared with the marketed CDDP preparation, the niosomes increased surviving fraction and reduced toxicity in the tumor-bearing rabbits. Moreover, the niosomes showed obvious predominance in inhibition of tumor growth and cell metastasis. Conclusion： The prepared CDDP niosomes have sustained release behavior, higher anti-tumor activity and lower toxicity.