用疏水改性的白及多糖制备载紫杉醇纳米粒并对其表征

成念; 赵文萃; 张琦; 王艳萍; 韩丹; 肖轩昂

doi:10.3969/j.issn.1006-0111.2017.01.012

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用疏水改性的白及多糖制备载紫杉醇纳米粒并对其表征

成念, 赵文萃, 张琦, 王艳萍, 韩丹, 肖轩昂

文章导航 > 药学实践与服务 > 2017 > 35(1): 48-53

成念, 赵文萃, 张琦, 王艳萍, 韩丹, 肖轩昂. 用疏水改性的白及多糖制备载紫杉醇纳米粒并对其表征[J]. 药学实践与服务, 2017, 35(1): 48-53. doi: 10.3969/j.issn.1006-0111.2017.01.012

引用本文:

CHENG Nian, ZHAO Wencui, ZHANG Qi, WANG Yanping, HAN Dan, XIAO Xuanang. Paclitaxel loaded nanoparticles with cholesterol succinyl bletilla striata polysaccharide as a carrier[J]. Journal of Pharmaceutical Practice and Service, 2017, 35(1): 48-53. doi: 10.3969/j.issn.1006-0111.2017.01.012

Citation:

CHENG Nian, ZHAO Wencui, ZHANG Qi, WANG Yanping, HAN Dan, XIAO Xuanang. Paclitaxel loaded nanoparticles with cholesterol succinyl bletilla striata polysaccharide as a carrier[J]. Journal of Pharmaceutical Practice and Service, 2017, 35(1): 48-53. doi: 10.3969/j.issn.1006-0111.2017.01.012

用疏水改性的白及多糖制备载紫杉醇纳米粒并对其表征

doi: 10.3969/j.issn.1006-0111.2017.01.012

1.
延边大学药学院, 吉林延吉 133000
2.
解放军208医院, 吉林长春 130062

Paclitaxel loaded nanoparticles with cholesterol succinyl bletilla striata polysaccharide as a carrier

1.
School of Pharmacy, Yan Bian University, Yanji 133000, China
2.
No. 208 Hospital of PLA, Changchun 130062, China

摘要: 目的讨论白及多糖作为药物递送载体的可行性。方法制备疏水性胆甾醇琥珀酰基白及多糖（CHSB）后，以紫杉醇（PTX）为模型药物，采用透析法制备载药纳米粒子，然后在透射电镜（TEM）下观察其形态；用动态光散射仪（DLS）检测其粒径、粒径分布和Zeta电位；用高效液相色谱法（HPLC）测定其包封率和载药量，并考察其体外释放情况；采用差示量热扫描法（DSC）确证药物在载药纳米粒子中的存在形式；采用MTT法考察纳米粒子的体外抗肿瘤活性，用荧光标记法观察肝癌细胞QGY-7703对纳米粒子的摄取情况。结果制备的纳米粒呈规则球形，粒度分布均匀，药物包载于纳米粒内部，载药量和包封率在一定范围受CHSB的影响，载药纳米粒对肝癌细胞的杀伤性强于游离药物，在细胞内可观察到罗丹明B标记的纳米粒呈现的荧光。结论 CHSB作为难溶性药物载体具有较高的可行性，因此可作为一种极具潜力的纳米载体材料。
- 白及多糖 /
- 疏水改性 /
- 紫杉醇 /
- 纳米粒 /
- 抗肿瘤
Abstract: Objective To explore the feasibility of bletilla striata polysaccharide as a drug delivery material. Method With hydrophobic cholesterol succinyl bletilla striata polysaccharide (CHSB) as the carrier, the model drug paclitaxel (PTX) loaded nanoparticles were prepared via dialysis method. The morphology of nanoparticles was observed by Transmission Electron Microscope (TEM). The particle size, distribution and zeta potential were characterized by Dynamic Light Scattering instrument (DLS). The entrapment efficiency, drug loading and in vitro release were determined by high performance liquid chromatography (HPLC). Differential Scanning Calorimetry (DSC) was used to confirm the drug form in the drug loaded nanoparticles. The in vitro antitumor activity of nanoparticles was assayed by MTT. The uptake of nanoparticles by QGY-7703 liver cancer cells was observed by fluorescence labeling method. Results The prepared nanoparticles had spherical shape with uniform particle size distribution. The drug was loaded in the interior of the nanoparticles. Drug loading and encapsulation efficiency were affected by the CHSB in certain range. The cytotoxicity of drug loaded nanoparticles on liver cancer cells was stronger than the free drug. The fluorescence of Rhodamine B labeled drug nanoparticles were observed in the cells. Conclusion Cholesterol succinyl bletilla striata polysaccharide (CHSB) is highly feasible as an insoluble drug carrier. It can be used as a potential Nano carrier material.
- bletilla striata polysaccharide /
- hydrophobic modification /
- Paclitaxel /
- nanoparticles /
- antitumor

[1]	孙达锋,史劲松,张卫明,等. 白及多糖胶研究进展[J].食品科学,2009,30(3):296.
[2]	毕亚静,王艳萍,刘福强,等. 胆甾醇琥珀酰基白及多糖的制备及其理化性质研究[J]. 药学实践杂志,2013,31(3):220-222.
[3]	赵雪竹,刘洋,王艳萍,等. 原料纯度对白及多糖疏水改性反应取代度的影响[J].药学实践杂志,2015,33(3):221-225.
[4]	杨文智. 疏水改性普鲁兰多糖及其自组装载药纳米粒的研究.北京:北京协和医学院,2009.
[5]	李磊. 胆固醇基-羧甲基可德兰衍生物自聚集纳米粒子的制备以及作为抗肿瘤药物载体的研究. 北京:中国协和医科大学,2010.
[6]	Gupta PN, Jain S, Nehate C,et al.Development and evaluation of paclitaxel loaded PLGA:poloxamer blend nanoparticles for cancer chemotherapy[J].Int J Biol Macromol,2014,69:393-399.
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用疏水改性的白及多糖制备载紫杉醇纳米粒并对其表征

doi: 10.3969/j.issn.1006-0111.2017.01.012

1. 延边大学药学院, 吉林延吉 133000

2. 解放军208医院, 吉林长春 130062

收稿日期: 2016-05-31
修回日期: 2016-09-29

关键词:

白及多糖 /

疏水改性 /

紫杉醇 /

纳米粒 /

抗肿瘤

摘要: 目的讨论白及多糖作为药物递送载体的可行性。方法制备疏水性胆甾醇琥珀酰基白及多糖（CHSB）后，以紫杉醇（PTX）为模型药物，采用透析法制备载药纳米粒子，然后在透射电镜（TEM）下观察其形态；用动态光散射仪（DLS）检测其粒径、粒径分布和Zeta电位；用高效液相色谱法（HPLC）测定其包封率和载药量，并考察其体外释放情况；采用差示量热扫描法（DSC）确证药物在载药纳米粒子中的存在形式；采用MTT法考察纳米粒子的体外抗肿瘤活性，用荧光标记法观察肝癌细胞QGY-7703对纳米粒子的摄取情况。结果制备的纳米粒呈规则球形，粒度分布均匀，药物包载于纳米粒内部，载药量和包封率在一定范围受CHSB的影响，载药纳米粒对肝癌细胞的杀伤性强于游离药物，在细胞内可观察到罗丹明B标记的纳米粒呈现的荧光。结论 CHSB作为难溶性药物载体具有较高的可行性，因此可作为一种极具潜力的纳米载体材料。

English Abstract

Paclitaxel loaded nanoparticles with cholesterol succinyl bletilla striata polysaccharide as a carrier

1. School of Pharmacy, Yan Bian University, Yanji 133000, China

2. No. 208 Hospital of PLA, Changchun 130062, China

Received Date: 2016-05-31
Rev Recd Date: 2016-09-29

Keywords:

Abstract: Objective To explore the feasibility of bletilla striata polysaccharide as a drug delivery material. Method With hydrophobic cholesterol succinyl bletilla striata polysaccharide (CHSB) as the carrier, the model drug paclitaxel (PTX) loaded nanoparticles were prepared via dialysis method. The morphology of nanoparticles was observed by Transmission Electron Microscope (TEM). The particle size, distribution and zeta potential were characterized by Dynamic Light Scattering instrument (DLS). The entrapment efficiency, drug loading and in vitro release were determined by high performance liquid chromatography (HPLC). Differential Scanning Calorimetry (DSC) was used to confirm the drug form in the drug loaded nanoparticles. The in vitro antitumor activity of nanoparticles was assayed by MTT. The uptake of nanoparticles by QGY-7703 liver cancer cells was observed by fluorescence labeling method. Results The prepared nanoparticles had spherical shape with uniform particle size distribution. The drug was loaded in the interior of the nanoparticles. Drug loading and encapsulation efficiency were affected by the CHSB in certain range. The cytotoxicity of drug loaded nanoparticles on liver cancer cells was stronger than the free drug. The fluorescence of Rhodamine B labeled drug nanoparticles were observed in the cells. Conclusion Cholesterol succinyl bletilla striata polysaccharide (CHSB) is highly feasible as an insoluble drug carrier. It can be used as a potential Nano carrier material.

引用本文:

Citation:

CHENG Nian, ZHAO Wencui, ZHANG Qi, WANG Yanping, HAN Dan, XIAO Xuanang. Paclitaxel loaded nanoparticles with cholesterol succinyl bletilla striata polysaccharide as a carrier[J]. Journal of Pharmaceutical Practice and Service, 2017, 35(1): 48-53. doi: 10.3969/j.issn.1006-0111.2017.01.012

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用疏水改性的白及多糖制备载紫杉醇纳米粒并对其表征

doi: 10.3969/j.issn.1006-0111.2017.01.012

Paclitaxel loaded nanoparticles with cholesterol succinyl bletilla striata polysaccharide as a carrier

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用疏水改性的白及多糖制备载紫杉醇纳米粒并对其表征

doi: 10.3969/j.issn.1006-0111.2017.01.012

1. 延边大学药学院, 吉林 延吉 133000 2. 解放军208医院, 吉林 长春 130062

English Abstract

Paclitaxel loaded nanoparticles with cholesterol succinyl bletilla striata polysaccharide as a carrier

1. School of Pharmacy, Yan Bian University, Yanji 133000, China 2. No. 208 Hospital of PLA, Changchun 130062, China

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目录

1. 延边大学药学院, 吉林延吉 133000

2. 解放军208医院, 吉林长春 130062

1. School of Pharmacy, Yan Bian University, Yanji 133000, China

2. No. 208 Hospital of PLA, Changchun 130062, China