生物素化壳聚糖修饰的PLGA纳米粒的制备及表征

高等学校化学学报 ›› 2010, Vol. 31 ›› Issue (8): 1682.

生物素化壳聚糖修饰的PLGA纳米粒的制备及表征

陈红丽¹, 唐红波², 杨文智², 陈汉², 王银松³, 梅林^4,5, 张彤², 熊青青², 张其清²

1. 新乡医学院生命科学技术系, 河南省遗传性疾病与分子靶向药物重点实验室培育基地, 新乡 453003;
2. 中国医学科学院生物医学工程研究所, 天津市生物材料重点实验室, 天津 300192;
3. 天津医科大学药学院, 天津 300070;
4. 清华大学深圳研究生院, 深圳 518055;
5. 大连医科大学药学院, 大连116027

收稿日期:2009-11-05 出版日期:2010-08-10 发布日期:2010-08-10
通讯作者: 陈红丽, E-mail: chenhlhl@126.com; 张其清, E-mail: zhangqiq@xmu.edu.cn
基金资助:
国家重大科学研究计划项目(批准号: 2006CB933300)和新乡医学院省级重点学科开放课题资助.

Preparation and Characterization of PLGA Nanospheres Surface Modified with Biotinylated Chitosan

CHEN Hong-Li^1*, TANG Hong-Bo², YANG Wen-Zhi², CHEN Han², WANG Yin-Song³, MEI Lin^4,5, ZHANG Tong², XIONG Qing-Qing², ZHANG Qi-Qing^2*

1. Henan Key Laboratory of Hereditary Disease and Molecular Target Drug Therapy(Cultivating Base), Department of Life Science and Technology, Xinxiang Medical University, Xinxiang 453003, China;
2. Institute of Biomedical Engineering, Chinese Academy of Medical Science, Peking Union Medical College, Tianjin 300192, China;
3. College of Pharmacy, Tianjin Medical University, Tianjin 300070, China;
4. The Shenzhen Key Lab of Gene and Antibody Therapy, Center for Biotech and Bio-Medicine and Division of Life Sciences, Graduate School at Shenzhen, Tsinghua University, Shenzhen 518055, China;
5. College of Pharmacy, Dalian Medical University, Dalian 116027, China

Received:2009-11-05 Online:2010-08-10 Published:2010-08-10
Contact: CHEN Hong-Li, E-mail: chenhlhl@126.com; ZHANG Qi-Qing, E-mail: zhangqiq@xmu.edu.cn
Supported by:
国家重大科学研究计划项目(批准号: 2006CB933300)和新乡医学院省级重点学科开放课题资助.

摘要/Abstract

摘要： 合成了生物素化壳聚糖(Bio-CS), 并通过核磁共振(¹H NMR)及电感耦合等离子体光质谱法(ICP-MS)对其进行结构确证. 采用溶剂挥发法(W₁/O/W₂)制备聚乳酸-羟基乙醇酸(PLGA)纳米粒, 并通过共价交联法对纳米粒进行Bio-CS表面修饰. 未修饰的PLGA纳米粒在扫描电镜下观察呈规则球状形态, 平均粒径为(248.4±21.0) nm, Zeta电势为-(21.21±2.13) mV, Bio-CS修饰后的PLGA纳米粒保持球状形态, 平均粒径为(268.3±23.4) nm, Zeta电势为(25.45±2.59) mV. 采用X射线光电子能谱(XPS)以及试剂盒对纳米粒表面生物素进行定性及定量研究, 结果显示, 经过Bio-CS修饰后的纳米粒表面含有N, S元素, 生物素取代度为31%的Bio-CS修饰的PLGA纳米粒, 其表面生物素含量为(1.36±0.34) μmol/100 mg纳米粒.

关键词: 纳米粒, 聚乳酸-羟基乙醇酸, 生物素化壳聚糖, 抗肿瘤

Abstract: Biotinylated chitosan(Bio-CS conjugates or Bio-CS) were synthesized and characterized. The degree of substitution(DS), as defined as the number of biotin per 100 anhydroglucose units of CS, was determined by ¹H NMR and ICP. Poly(lactic-co-glycolic acid)(PLGA) nanospheres were prepared by a solvent evaporation technique(W₁/O/W₂). The surface of PLGA nanosphere was modified with Bio-CS by covalent binding. PLGA nanospheres were almost spherical in shape under the scanning electron microscopy(SEM) observation, and their mean diameter determined by the laser light scattering technique was (248.4±21.0) nm. Bio-CS modified PLGA nanospheres were also spherical in shape; their mean diameter and Zeta potential value were (268.3±23.4) nm and -(21.21±2.13) mV, respectively. The surface chemistry of nanospheres was quantitatively studied by X-ray photoelectron spectroscopy(XPS). The results show the N region corresponding to the primary amide of CS and the S region corresponding to the biotin, indicating that PLGA nanospheres were successfully surface-modified with Bio-CS. The content of biotin on the surface of Bio-CS modified PLGA nanospheres with DS of biotin of 31% was determined using a commercially available Quant*TagTM Biotin Kit and its value was (1.36±0.34) mol/100 mg.

Key words: Nanoparticle, Poly(lactic-co-glycolic acid)(PLGA), Biotinylated chitosan anticancer

TrendMD:

陈红丽, 唐红波, 杨文智, 陈汉, 王银松, 梅林, 张彤, 熊青青, 张其清. 生物素化壳聚糖修饰的PLGA纳米粒的制备及表征. 高等学校化学学报, 2010, 31(8): 1682.

CHEN Hong-Li*, TANG Hong-Bo, YANG Wen-Zhi, CHEN Han, WANG Yin-Song, MEI Lin, .... Preparation and Characterization of PLGA Nanospheres Surface Modified with Biotinylated Chitosan. Chem. J. Chinese Universities, 2010, 31(8): 1682.

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