斑蝥素载药胶束的制备及其体外释药性能考察

李真真; 岳巧欣; 王杰; 臧琛; 易红; 李鹏岳; 赵庆贺; 陈燕军

doi:10.13422/j.cnki.syfjx.2016240005

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斑蝥素载药胶束的制备及其体外释药性能考察

药剂与炮制 | 更新时间：2024-01-04

- 斑蝥素载药胶束的制备及其体外释药性能考察
- Preparation of Cantharidin Loaded Polymer Micelles and Investigation of Its Release Properties
- 中国实验方剂学杂志 2016年22卷第24期页码：5-8
- 作者机构：
- 作者简介：
- 基金信息：
  
  国家“重大新药创制”科技重大专项（2014ZX09304307001）;北京市自然科学基金项目（2152036）
- DOI：10.13422/j.cnki.syfjx.2016240005
  中图分类号： R283.6
- 纸质出版日期：2016
- 稿件说明：
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李真真, 岳巧欣, 王杰, 等. 斑蝥素载药胶束的制备及其体外释药性能考察[J]. 中国实验方剂学杂志, 2016,22(24):5-8.

LI Zhen-zhen, YUE Qiao-xin, WANG Jie, et al. Preparation of Cantharidin Loaded Polymer Micelles and Investigation of Its Release Properties[J]. Chinese journal of experimental traditional medical formulae, 2016, 22(24): 5-8.
李真真, 岳巧欣, 王杰, 等. 斑蝥素载药胶束的制备及其体外释药性能考察[J]. 中国实验方剂学杂志, 2016,22(24):5-8. DOI： 10.13422/j.cnki.syfjx.2016240005.

LI Zhen-zhen, YUE Qiao-xin, WANG Jie, et al. Preparation of Cantharidin Loaded Polymer Micelles and Investigation of Its Release Properties[J]. Chinese journal of experimental traditional medical formulae, 2016, 22(24): 5-8. DOI： 10.13422/j.cnki.syfjx.2016240005.

摘要

目的：制备pH敏感斑蝥素聚合物胶束纳米制剂，以提高斑蝥素在水中的溶解度，并考察该制剂在弱酸性条件下的体外释药特性。方法：以聚乙二醇-聚乳酸共聚物[poly（ethylene glycol）-b-polylactide，PELA]和聚乙二醇-聚乳酸-聚（β-氨基酯）[poly（ethylene glycol）-b-polylactide-b-poly（β-amino ester），PELA-PBAE]为载体，采用薄膜水化法制备斑蝥素胶束。通过透射电子显微镜观察胶束的微观形态，采用粒度分析仪测定粒径，HPLC测定其载药量和包封率，透析袋透析法测定纳米胶束在不同pH条件下的释放特性。结果：斑蝥素胶束呈明显的球状结构，PELA载药（PELA-C）胶束和PELA-PBAE载药（PELA-PBAE-C）胶束的粒度分别为21.6，21.2 nm，且至少在5 d内稳定；载药量分别为1.68%和1.72%，包封率分别为92.0%和88.8%；在pH 5.5下的8 h累计释放率分别为24.7%和79.1%，在pH 6.5下的8 h累计释放率分别为13.6%和50.0%，在pH 7.4下的8 h累计释放率分别为10.2%和13.9%。结论： PELA-PBAE作为纳米载体能明显提高斑蝥素的水溶性，体外释药具有显著的pH响应性能，在抗肿瘤药物的开发方面具有较好的应用前景。

Abstract

Objective: pH responsive polymer micelles loaded with cantharidin were prepared to increase the solubility of cantharidin in water.The pH responsive property of the micelles was verified by the controlled drug release under tumoral mimic mild acidic environment. Method: Cantharidin micelles were prepared by thin film hydration method with amphiphilic methoxy poly(ethylene glycol)-b-polylactide (PELA) block copolymer and methoxy poly(ethylene glycol)-b-polylactide-b-poly(β-amino ester) (PELA-PBAE) as carriers.The structure and morphology of the micelles was characterized by transmission electron microscopy.The particle size of the micelles was measured by laser light scattering analyzer.HPLC was employed to determine drug loading and encapsulation efficiency of the micelles.In vitro release of the micelles was performed in phosphate buffered saline (pH of 7.4

6.5 and 5.5

respectively) by permeation diffusion method. Result: The micelles of PELA-cantharidin (PELA-C) and PELA-PBAE-C exhibited spherical shape with particle size of 21.6 nm and 21.2 nm

respectively;they were at least stable within 5 d.Drug loading and encapsulation efficiency of PELA-C micelles were 1.68% and 92.0%

while these of PELA-PBAE-C micelles were 1.72% and 88.8%

respectively.The cumulative release rates of PELA-C micelles and PELA-PBAE-C micelles in 8 h were 24.7% and 79.1% under pH of 5.5

13.6% and 50.0% under pH of 6.5

10.2% and 13.9% under pH of 7.4

respectively. Conclusion: The solubility of cantharidin is significantly improved with PELA-PBAE as nanocarrier

in vitro release of PELA-PBAE-C micelles has significant pH responsive performance.

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