用疏水改性的白及多糖制备载紫杉醇纳米粒并对其表征

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

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。

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 in strument （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 nan oparticles. The in vitro antitumor activity of nanoparticles was assayed by MTT. The uptake of nanoparticles by QGY-7703 liver cancer ceils 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 nanopartieles 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 suceinyl bletilla striata polysaccharide （CHSB） is highly feasible as an insoluble drug carrier. It can be used as a potential Nano carrier material.