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目的:硫酸长春新碱作为一种细胞毒型抗肿瘤药物,临床上多用其注射剂,虽应用广泛,但存在较多缺点,如药物半衰期短,代谢速率快以及毒副作用明显。本文目的是制备包载长春新碱和十二烷基磺酸钠的阳离子纳米结构脂质载体,并对其进行评价。方法:用复乳挥发法制备出目标脂质纳米粒;利用激光粒度仪对其粒径及zeta电位进行检测;利用高效液相色谱法对其包封率和载药量进行测定;透析法检测纳米粒的体外释放行为;用小肠吸收法评价纳米粒的促进吸收作用。结果:制得的纳米粒的平均粒径为(192.4±4.14)nm,多分散系数(PDI)为0.184±0.015,包封率为32.28%,Zeta电位为(30.6±4.09)m V,载药量为(1.56±0.10)%;体外释放实验显示在pH=7.4的中性释放介质中,硫酸长春新碱脂质纳米粒表现出缓释特性;小肠吸收实验表明十二烷基磺酸钠的加入和阳离子纳米粒的修饰可提高小肠对药物的吸收。结论:阳离子硫酸长春新碱纳米结构脂质载体具有缓释效果,并可以促进小肠对药物的吸收。
OBJECTIVE: Vincristine sulfate is a kind of cytotoxic anti-tumor drugs. It is widely used in clinic. Although it is widely used, it has many shortcomings such as short half-life of drug, fast metabolic rate and obvious side effects. The purpose of this paper is to prepare and evaluate cationic nanostructured lipid carriers containing vincristine and sodium dodecyl sulfate. Methods: The target lipid nanoparticles were prepared by double emulsion evaporation method. The particle size and zeta potential were detected by laser particle size analyzer. The entrapment efficiency and drug loading were determined by high performance liquid chromatography (HPLC) The in vitro release behavior of nanoparticles was evaluated by the intestinal absorption method. Results: The average diameter of the prepared nanoparticles was (192.4 ± 4.14) nm, the PDI was 0.184 ± 0.015, the entrapment efficiency was 32.28% and the Zeta potential was (30.6 ± 4.09) m V. (1.56 ± 0.10)%; in vitro release experiments showed that vinblastine sulfate lipid nanoparticles showed sustained release characteristics in a neutral release medium pH = 7.4; intestinal absorption experiments showed that sodium dodecyl sulfate Addition and modification of cationic nanoparticles can increase the intestinal absorption of drugs. CONCLUSION: The cationic vincristine sulfate nanostructured lipid carrier has sustained release effect and can promote intestinal absorption of drugs.