PEG修饰的紫杉醇固体脂质纳米粒的制备及其性质研究  

Preparation and characters investigation of PEG modified paclitaxel solid lipid nanoparticles

作　　者：郑洁[1] 万瑜[1] 樊戈睿 孙逊[1] 

机构地区：[1]四川大学华西药学院靶向药物与释药系统教育部重点实验室,四川成都610041

出　　处：《华西药学杂志》2014年第3期234-236,共3页West China Journal of Pharmaceutical Sciences

摘　　要：目的制备PEG修饰的固体脂质纳米粒,并研究其性质。方法采用薄膜超声法制备包载紫杉醇的固体脂质纳米粒,再利用EDC/NHS脱水缩合法在纳米粒表面进行PEG修饰,得到PEG修饰的固体脂质纳米粒。用苦味酸-分光光度法测定PEG的含量;用透射电镜考察纳米粒的形态特点;采用凝胶柱洗脱联合HPLC测定包封率;筛选纳米粒的最佳冻干条件。结果成功制备了PEG修饰的紫杉醇固体脂质纳米粒,通过脱水缩合法连接到纳米粒上的PEG化多肽占加入总量的26.5%;紫杉醇固体脂质纳米包封率为75%,载药量为7%。结论制备的PEG修饰的紫杉醇固体脂质纳米粒具有较整齐的外观形态、较高载药量和较好的稳定性。OBJECTIVE To prepare the PEG modified paclitaxel （PTX） solid lipid nanoparticles （SLNs） and study its properties. METHODS The PTX loaded SLNs were prepared by the thin film hydration and sonieation dispersion technique. The EDC/NHS dehydration method was applied to link the PEG - peptide to the SLNs. The morphous of SLNs was observed by TEM and the encapsulation efficiency of SLNs was determined by the sephadex gel column and HPLC method. The conjugation efficiency of PEG - peptide（Pp） on the surface of SLNs were determined by bitter acid spectrophotometric method. The freeze drying condition was also screened. RESULTS The Pp - PTX - SLNs were prepared successfully. The PEG - peptides successfully conjugated to SLNs accounted for 26. 5% of the total. The encapsulation efficiency of SLNs was 75% and the drug loading was 7%. CONCLUSION Pp - PTX- SLNs preparated by the thin film hydration and sonication dispersionn technique exhibit high encapsulation efficiency, fine morphous and stability.

关 键 词：PEG修饰 紫杉醇 固体脂质纳米粒 苦味酸-分光光度法 

分 类 号：R94[医药卫生—药剂学]