摘要
制备了硬脂酸改性白芨多糖两亲性聚合物(SA-BSPS)药物载体,采用红外光谱及核磁共振氢谱对SA-BSPS药物载体进行了表征,并以核磁共振氢谱峰面积计算取代度.以多西他赛(DTX)为模型药物,制备了多西他赛-硬脂酸改性白芨多糖聚合物(DTX-SA-BSPS)胶束,测定了DTX-SA-BSPS的粒径分布、Zeta电位、载药量及包封率.结果表明,硬脂酸已接枝到白芨多糖的羟基上,取代度为12.94%.DTX-SA-BSPS胶束的粒径为(97.01±3.17)nm,Zeta电位为(-19.56±0.22)m V,载药量为(9.13±0.17)%、包封率达(81.11±0.18)%.探讨了SA-BSPS胶束的细胞毒性及其被人肝癌细胞(Hep G2)株摄入的情况.细胞毒性实验表明,浓度为0.5μg/m L的SA-BSPS胶束孵育72 h时,肝癌细胞存活率为(78.82±3.25)%.荧光摄入实验表明,孵育4 h后细胞中包载罗丹明B的SA-BSPS胶束的荧光强度明显强于游离罗丹明B,且在孵育过程中,荧光强度随孵育时间的延长而增强.
Stearic acid（ SA）-modified Bletilla Striata polysaccharides（ BSPS） amphiphilic copolymers（ SA-BSPS） were prepared. Fourier transform infrared spectroscopy and1 H nuclear magnetic resonance spectroscopy（1H NMR） were used to describe SA-BSPS group. The substitued degree of the SA-BSPS group was determined by the peak area oflH NMR. Docetaxel-loaded SA-conjugated BSPS（ DTX-SA-BSPS） copolymer micelles were formulated and characterized in terms of particle diameter,Zeta potential,drug loading capacity（ LC） and encapsulation efficiency（ EE）. Further,the uptake of rhodamine B-labeled SA-BSPS copolymer micelles and antitumor activity in vitro on human liver cancer cell line（ Hep G2） were carried out. The results indicated that SA was successfully conjugated with BSPS and the substitued degree of the SA-BSPS group was12. 94%. DTX-SA-BSPS copolymer micelles had an average size of（ 97. 01 ±3. 17） nm with Zeta potential in the range of（-19. 56 ±0. 22） mV. The drug encapsulation and loading capacity were（ 81. 11 ±0. 18） % and（ 9. 13 ± 0. 17） % respectively. The average cell line viability of blank SA-BSPS polymer micelles were（ 78. 82±3. 25） % at 0. 5 μg /mL after 72 h incubation. Fluorescent intensity of Hep G2 cells incubated for 4 h with rhodamine B-labeled SA-BSPS copolymer micelles was higher than that of rhodamine B and fluorescent intensity exhibited an increase trend when incubation time were prolonged.
作者
管清香
张广远
孙丹丹
孙士淋
孙诚
刘昕
韩冰
GUAN Qingxiang ZHANG Guangyuan SUN Dandan SUN Shilin SUN Cheng LIU Xin HAN Bing(School of Pharmacy, Jilin University, Changchun 130021, China)
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
2016年第10期1915-1920,共6页
Chemical Journal of Chinese Universities
基金
国家自然科学基金(批准号:81401513)
吉林大学研究生创新基金(批准号:2016225)资助~~
关键词
白芨多糖
两亲性聚合物
聚合物胶束
载药量
包封率
Bletilla Striata polysaccharide
Amphiphilic copolymer
Polymer micelle
Drug loading capacity
Encapsulation efficiency
