RGD-FasL羟乙基壳聚糖缓释纳米粒制备及生物学研究  

Preparation and bioactivities assaying of RGD-FasL glycol chitosan based nanoparticles

作　　者：刘彬[1,2] 张晶[3] 杨晶晶[1] 黄小平[1] 张敏萍[1] 罗芳洪[1] 庄国洪[1] 

机构地区：[1]厦门大学医学院抗癌中心,福建厦门361005 [2]汕头市卫生学校药学教研室,广东汕头515073 [3]厦门市第二医院检验科,福建厦门361024

出　　处：《中国生化药物杂志》2012年第6期772-775,共4页Chinese Journal of Biochemical Pharmaceutics

基　　金：福建省公益基金资助项目(NO.2011R1039-2)

摘　　要：目的使用羟乙基壳聚糖制备纳米颗粒(NPs),用来包载RGD-FasL融合蛋白(RF),鉴定其功能并评估其在肝癌治疗中的作用。方法采用离子凝胶法制备RF羟乙基壳聚糖缓释纳米粒(RF-NPs);通过透射电镜、动态光散射法考察其理化性质;用紫外分光光度仪检测蛋白浓度来计算其载药率、包封率和体外释放度;通过MTT比色法检测对H22细胞增殖活性的影响,应用H22细胞建立小鼠肝癌模型进行体内抑瘤研究。结果制备的RF-NPs呈球形或类球形,平均粒径198.3 nm,Zeta电位+25 mV,包封率较高,且具有缓释效果,150 mg/L浓度时对H22细胞抑制率大于70%,并能在小鼠体内产生比较明显的抑瘤效果。结论离子凝胶法制备RF-NPs的条件缓和、方法简单,是癌症治疗中具有很好的前景的蛋白药物载体。Purpose To prepare nanoparticles for encapsulating RGD-FasL with glycol chitosan and to evaluate the functions of nanoparticles and the roles in therapy for cancer of the liver. Methods RGD- FasL glycol chitosan based nanopartieles （RF-NPs） were prepared by ionic gelation method. The physic- chemical properties were determined by the way of TEM and DLS. The release behaviour in vitro was de- termined. The encapsulation efficiency and loading rate of RF-NPs were examined with ultraviolet spectro- photometer. H22 Cell proliferative activity was examined by MTT. Anticancer effeet of the H22 hepatoma model established in mice was evaluated. Results The obtained RF-NPs were approximately spherical in shape with average particle size of 198.3 nm,Zeta potentials of ＋ 25 mV. When RF-NPs concentration was to 150 mg/L,its H22 tumor inhibitory rate can be over 70% in vivo. Also RF-NPs showed obvious tumor inhibiting effect and manifested sustained-release of RF in vitro. Conclusion RGD-FasL-NPs pre- pared by ionic gelation method was simple with mild preparing conditions and had the potential to make cancer therapy in vivo achievable.

关 键 词：纳米粒 RGD—FasL H22 

分 类 号：TQ460.6[化学工程—制药化工] R960[医药卫生—药理学]