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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 cisplatin vesicles and evaluate their physicochemical properties and anti-cancer activity. Methods: The vesicles were prepared by using Span40 and cholesterol as the main materials. Physical and chemical properties such as surface morphology, particle size distribution, potential, entrapment efficiency, drug loading and in vitro release characteristics were investigated. Body weight changes, survival rate, tumor growth and tumor cell metastasis in experimental rabbits. Results: The diameter of the vesicles was (7.33 ± 1.05) μm, the encapsulation efficiency was (86.06 ± 1.46)%, the drug loading was (3.04 ± 0.05)% and the release rate t1 / 2 was around 8 h . Compared with the commercially available preparation, the survival rate is greatly increased, the toxicity is obviously smaller, and the advantages in inhibiting tumor growth and preventing tumor cell metastasis are very obvious. Conclusion: The vesicles developed in this experiment have the characteristics of sustained release and high efficiency and low toxicity for the treatment of tumors.