葡萄糖修饰脑靶向紫杉醇脂质体包封率测定方法的比较

聂华; 赵莹; 叶小玲; 丘明建; 廖勇涛; 何志龙; 张声源

doi:10.13422/j.cnki.syfjx.2016230015

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葡萄糖修饰脑靶向紫杉醇脂质体包封率测定方法的比较

药剂与炮制 | 更新时间：2024-01-04

- 葡萄糖修饰脑靶向紫杉醇脂质体包封率测定方法的比较
- Comparison of Determination for Entrapment Efficiency of Paclitaxel-loaded Brain Targeting Liposomes
- 中国实验方剂学杂志 2016年22卷第23期页码：15-19
- 作者机构：
- 作者简介：
- 基金信息：
  
  广东省医学科研基金项目（A2015629）;广东省省级科技计划项目（2014A020221061）;广东省医学科研基金项目（A2015354）
- DOI：10.13422/j.cnki.syfjx.2016230015
  中图分类号： R943
- 纸质出版日期：2016
- 稿件说明：
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聂华, 赵莹, 叶小玲, 等. 葡萄糖修饰脑靶向紫杉醇脂质体包封率测定方法的比较[J]. 中国实验方剂学杂志, 2016,22(23):15-19.

NIE Hua, ZHAO Ying, YE Xiao-ling, et al. Comparison of Determination for Entrapment Efficiency of Paclitaxel-loaded Brain Targeting Liposomes[J]. Chinese journal of experimental traditional medical formulae, 2016, 22(23): 15-19.
聂华, 赵莹, 叶小玲, 等. 葡萄糖修饰脑靶向紫杉醇脂质体包封率测定方法的比较[J]. 中国实验方剂学杂志, 2016,22(23):15-19. DOI： 10.13422/j.cnki.syfjx.2016230015.

NIE Hua, ZHAO Ying, YE Xiao-ling, et al. Comparison of Determination for Entrapment Efficiency of Paclitaxel-loaded Brain Targeting Liposomes[J]. Chinese journal of experimental traditional medical formulae, 2016, 22(23): 15-19. DOI： 10.13422/j.cnki.syfjx.2016230015.

摘要

目的：建立葡萄糖修饰脑靶向紫杉醇脂质体的包封率测定方法，为该制剂的质量控制提供参考。方法：采用薄膜分散法制备脂质体。采用RP-HPLC测定紫杉醇的含量，流动相甲醇-水（70：30），检测波长228 nm，流速0.8 mL·min-1。利用RP-HPLC测定胆固醇的含量，流动相甲醇，检测波长210 nm，流速1 mL·min-1。采用凝胶柱色谱法、鱼精蛋白沉淀法、滤膜法、透析法分离脂质体与游离药物，比较4种方法测定包封率的可行性。结果：紫杉醇与胆固醇含量测定方法的专属性、精密度、稳定性和回收率试验均符合测定要求，线性范围分别为0.4~100，1~500 mg·L-1。4种方法紫杉醇与脂质体回收率均介于95%~105%，满足脂质体包封率测定的要求；包封率分别为74.68%，92.91%，95.14%，95.08%。结论：鱼精蛋白沉淀法操作简单、快捷，几乎不受脂质体粒径的影响，适用于紫杉醇脂质体包封率的测定。

Abstract

Objective: To establish a method for the determination of entrapment efficiency of glucose-modified paclitaxel-loaded brain targeting liposomes. Method: The liposomes were prepared by film dispersion method.The content of paclitaxel was detected by RP-HPLC with mobile phase of methanol-water (70:30)

detection wavelength at 228 nm and flow rate of 0.8 mL·min-1.The content of cholesterol was determined by RP-HPLC with mobile phase of methanol

detection wavelength at 210 nm and flow rate of 1.0 mL·min-1.The separation of free paclitaxel and liposomes was performed with gel column chromatography

protamine precipitation

filter membrane method and dialysis method to compare their feasibility for determination of entrapment efficiency. Result: The specificity

RSD of precision

stability and recovery test of both chromatographic methods for paclitaxel and cholesterol all met the demand of determination.Linear ranges of paclitaxel and cholesterol were 0.4-100

1-500 mg·L-1

respectively.Recoveries of paclitaxel and liposomes from four methods were all 95%-105%

which met the requirement of determination of entrapment efficiency.Entrapment efficiencies in gel column chromatography

protamine precipitation

filter membrane method and dialysis method were 74.68%

92.91%

95.14% and 95.08%. Conclusion: Protamine precipitation method is hardly affected by particle size of the liposomes

it is suitable for determination of entrapment efficiency of paclitaxel liposomes.

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