摘要
目的:制备一种新型的长循环紫杉醇脂质体,评价其质量,并考察对胃癌细胞(BGC823)的抑制作用。方法:实验于2006-05/11在凯里学院化学系实验室和黔东南州疾病预防控制中心理化科检验室进行。①包封率测定:采用超声薄膜法制备紫杉醇脂质体,用RP-HPLC测定紫杉醇脂质体的药物包封率。②稳定性测定:将紫杉醇脂质体分散在pH为6.5的磷酸缓冲液里,存放在4℃冰箱中30d,观察其包裹量的变化。③对胃癌细胞(BGC823)的抑制作用:MTT法考察在5,10,15,20mg/L4个不同药物浓度下,紫杉醇脂质体对处在对数生长期的BGC823细胞增殖的影响,并用紫杉醇游离药物作为对照。结果:①经RP-HPLC检测,这种长循环紫杉醇脂质体的药物包封率高达97.6%。②紫杉醇脂质体存放在4℃冰箱中,在长达1个月时间内不见絮凝状沉淀,在保存3,8,15,22,30d后,药物在脂质体颗粒中的包裹量分别为97.3%,96.2%,95.6%,94.9%和94.2%,在30d时间里紫杉醇脂质体在缓冲液中的药物泄漏仅有6%。③体外细胞毒性实验表明,5,10,15,20mg/L的紫杉醇注射液对BGC823细胞的抑制率分别为35.24%,48.37%,57.49%,74.84%,而相同药物浓度下的紫杉醇脂质体对BGC823细胞的抑制率为33.46%,44.15%,51.94%,68.64%。结论:①实验置备的紫杉醇脂质体实现了药物的高包封率,而且非常稳定。②紫杉醇药物浓度相同条件下,紫杉醇脂质体对BGC823细胞的抑制率低于游离的紫杉醇药物,说明脂质体对紫杉醇起到了一个很好的缓释作用。
AIM： To prepare a novel long-circulating paclitaxel-containing liposomes, evaluate its quality and study its toxicity to gastric cancer cell line BGC823. METHODS： From May to November in 2006, the experiment was carried out in the Laboratory of Chemistry, Kaili College and the Laboratory of Physics and Chemistry Department, Southeast Guizhou Center for Disease Control and Prevention. ①The novel long-circulating paclitaxel-containing liposomes was prepared by ultrasonic film method. Encapsulation efficiency and stability of the paclitaxel liposomes were measured by RP-HPLC.②The paclitaxel liposomes were dispersed in phosphate buffer at the pH value of 6.5, at 4 % for 30 days, and the change of drug loads was observed. ③The proliferation of BGC823 cell at logarithmic phase was tested by MTT method under the paclitaxel liposomes concentrations of 5, 10, 15, 20 mg/L. Meanwhile the paclitaxel free drug was taken as controls. RESULTS： ①Encapsulation efficiency of this paclitaxel liposomes was high to 97.6% detected by RP-HPLC②When the paclitaxel liposomes were stored in refrigerator of 4 %, there was no flocculent precipitation during one month. Drug loaded in liposome after 3, 8, 15, 22, 30 days of preservation was respectively 97.3%, 96.2%, 95.6%, 94.9%, and 94.2%. The drug leakage of the paclitaxel liposomes was only 6% one month after dispersing in this buffer. ③The result of in vitro cell toxicity showed that, under the drug concentration of 5, 10, 15, 20 mg/L, the inhibition rate to BGC823 cell of paclitaxel liposomes was 33.46%, 44.15%, 51.94%, 68.64% respectively, where those of free paclitaxel was 35.24%, 48.37%, 57.49%, 74.64%. CONCLUSION：①This high-encapsulated and stable long-circulating paclitaxel-containing liposomes is expected to provide a more effective paclitaxel preparation.②The inhibition rate to BGC823 cell of the paclitaxel liposomes is low to that of free paclitaxel at the same drug concentration, indicating that it can present the slow release of liposomes.
出处
《中国组织工程研究与临床康复》
CAS
CSCD
北大核心
2007年第26期5113-5116,共4页
Journal of Clinical Rehabilitative Tissue Engineering Research
