中国组织工程研究 ›› 2012, Vol. 16 ›› Issue (3): 421-425.doi: 10.3969/j.issn.1673-8225.2012.03.009

• 纳米生物材料 nanobiomaterials • 上一篇    下一篇

聚乳酸/聚乙二醇琥珀酸酯-姜黄素纳米粒的制备及体外评价*★

潘艺茗,黄岳山   

  1. 华南理工大学生物医学工程系,广东省广州市 510006
  • 收稿日期:2011-05-18 修回日期:2011-07-14 出版日期:2012-01-15 发布日期:2012-01-15
  • 作者简介:潘艺茗★,女,1988年生,陕西省渭南市人,汉族,华南理工大学在读硕士,主要从事生物材料药物载体研究。 pym200888@ 126.com
  • 基金资助:

    广东省自然科学基金项目(9151052005000006)。

Preparation and in vitro evaluation of poly(lactide)/tocopheryl polyethylene glycol succinate-curcumin nanoparticles

Pan Yi-ming, Huang Yue-shan   

  1. Department of Biomedical Engineering, South China University of Technology, Guangzhou  510006, Guangdong Province, China
  • Received:2011-05-18 Revised:2011-07-14 Online:2012-01-15 Published:2012-01-15
  • About author:Pan Yi-ming★, Studying for master’s degree, Department of Biomedical Engineering, South China University of Technology, Guangzhou 510006, Guangdong Province, China pym200888@ 126.com
  • Supported by:

    the Natural Science Foundation of Guangdong Province, No. 9151052005000006*

摘要:

背景:聚乳酸及其共聚物是一类具有良好生物相容性的可降解高分子材料,已被广泛用于可生物降解型药物缓释或靶向给药系统中。
目的:探索载药纳米粒制备条件对包封率和载药量的影响,确定最佳制备工艺条件。
方法:以维生素E1000聚乙二醇琥珀酸酯(TPGS)为乳化剂、姜黄素为模型药物、聚乳酸为载体材料,采用O/W型乳化-溶剂挥发法制备聚乳酸-姜黄素纳米粒,以包封率和载药量为主要指标,单因素实验探索影响两指标的主要因素,再正交试验设计优化制备工艺。
结果与结论:通过正交试验设计制备聚乳酸-姜黄素纳米粒的最佳工艺为:水油相比10∶1,聚合物浓度15 g/L,药物浓度3 g/L,乳化剂TPGS浓度0.03%。以此工艺制备的载药纳米粒外形圆整光滑,粒度分布较为均匀,平均粒径为167.5 nm,包封率为89.52%,载药量为13.72%,纳米粒前期突释不明显具有良好的缓释作用。该工艺稳定、简单可行,优化制备工艺得到的聚乳酸-姜黄素纳米粒粒径适中、包封率和载药量较高。

关键词: 姜黄素, 聚乳酸, 纳米粒, 正交实验, 缓释

Abstract:

BACKGROUND: Poly(lactide) (PLA) and its copolymer are a class of biodegradable polymer materials with good biocompatibility, which have been widely used for biodegradable sustained release drugs or targeted drug delivery systems.
OBJECTIVE: To explore the preparation method of the drug-loaded nanoparticles on entrapment rates (ER) and drug loading (DL) efficiency, and to determine the optimal preparation conditions using tocopheryl polyethylene glycol succinate (TPGS) as emulsifier, curcumin as a model drug and PLA as carriers.
METHODS: Curcumin loaded PLA nanoparticles (NPs) were prepared by an O/W emulsion-solvent evaporation method. The ER and DL were used as the main guiders. Singe factor test was used in order to find the effect of all kinds of parameters on the NP’s preparation, and then NP’s formulations were optimized by orthogonal design test.
RESULTS AND CONCLUSION: The optimal preparation conditions of NPs were determined through orthogonal experiment. The optimal technique parameters were followed: water to organic ratio of 10:1, polymer concentration of 15 g/L, drug concentration of 3 g/L, emulsifier TPGS concentration of 0.03%. NPs prepared under the optimum condition were spherical and smooth with narrow particle size distribution and sustained drug release. The mean diameter was 167.5 nm, the ER was 89.52%, and the DL was 13.72%. This preparation process is stable, simple and feasible, and the NPs with a highly ER, DL, and uniform size distribution can be prepared under optimal preparation conditions.
 

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