摘要
背景:紫杉醇是临床常用的广谱抗肿瘤植物药,但其不良反应较多,因此迫切需要合适的载体以减小紫杉醇本身的毒性,同时达到更好的靶向性。目的:研究表皮生长因子偶联牛血清白蛋白纳米粒荷载紫杉醇的制备及其理化性质的鉴定。方法:采用超声乳化和溶剂挥发技术制备白蛋白纳米粒,通过化学交联试剂将表皮生长因子与白蛋白纳米粒偶联,制得表皮生长因子偶联白蛋白纳米粒,使用表皮生长因子偶联白蛋白纳米粒荷载125I标记紫杉醇,作为实验样品。在白蛋白纳米粒与表皮生长因子偶联白蛋白纳米粒中分别加入100,200,400,800 mg/L的125I标记紫杉醇,进行包封率和载药量检测;检测实验样品、荷载125I标记紫杉醇白蛋白纳米粒的药物释放率;检测实验样品、荷载125I标记紫杉醇白蛋白纳米粒与125I标记紫杉醇的室温稳定性及血清稳定性。结果与结论:荷载125I标记紫杉醇的白蛋白纳米粒组和实验样品组的包封率和载药量随着紫杉醇药量的增加,包封率呈现下降趋势,载药量呈现上升趋势。实验样品、荷载125I标记紫杉醇白蛋白纳米粒释药趋势基本相同,表现为包载药物缓慢释放。实验样品、荷载125I标记紫杉醇白蛋白纳米粒的室温稳定性与血清稳定性均高于125I标记紫杉醇(P<0.05)。表明表皮生长因子偶联白蛋白纳米粒荷载紫杉醇具有良好的载药率、释药率和稳定性。
BACKGROUND： Paclitaxel is a broad-spectrum antitumor plant drug commonly used, possessing much adverse reactions. Therefore, there is an urgent need for an appropriate carrier to reduce the toxicity of paclitaxel, and achieve better targeting.
OBJECTIVE： To explore the preparation of epidermal growth factor （EGF） coupling bovine serum albumin nanoparticles loading paclitaxel and its physical and chemical properties.
METHODS： Albumin nanoparticles were prepared by phacoemulsification and solvent evaporation technology, and EGF was coupled with albumin nanoparticles by chemical crosslinking reagents. The EGF coupling albumin nanoparticles loading 125I marked paclitaxel acted as experimental samples. 100, 200, 400, 800 mg/L 125I marked paclitaxel was added to albumin nanoparticles and EGF coupling albumin nanoparticles respectively for detection of encapsulation efficiency and loading rate. The drug releasing rate of samples and albumin nanoparticles loading 125I marked paclitaxel were measured. The stability at room temperature and serum stability of samples, albumin nanoparticles loading 125I marked paclitaxel and 125I marked paclitaxel were detected.
RESULTS AND CONCLUSION： With the increasing of paclitaxel dosage, in albumin nanoparticles loading 125I marked paclitaxel group and experimental sample group, the encapsulation efficiency showed a trend of decline but the drug loading rate presented a rising tendency. Experimental sample group and albumin nanoparticles loading 125I marked paclitaxel group showed the same releasing drug trend basically, manifesting the sustained release of paclitaxel. The stability at room temperature and serum stability of experimental sample group and albumin nanoparticles loading 125I marked paclitaxel group were both higher than those in 125I marked paclitaxel group （P 〈 0.05）. From what has been discussed above, EGF coupling albumin nanoparticles loading 125I marked paclitaxel have good drug-loading rate, drug release rate and stability.
出处
《中国组织工程研究》
CAS
CSCD
2014年第52期8393-8398,共6页
Chinese Journal of Tissue Engineering Research
基金
国家自然科学基金(30070230
30424005)~~
