中国组织工程研究

中国组织工程研究 ›› 2011, Vol. 15 ›› Issue (8): 1389-1391.doi: 10.3969/j.issn.1673-8225.2011.08.014

• 药物控释材料 drug delivery materials • 上一篇    下一篇

全反式维甲酸-聚酸酐长效缓释剂研制及其可行性

于美丽，杜  智，郭宏玥，孙金芳，杜  雪   

  1. 天津市第三中心医院肝胆疾病重点实验室，天津市  300170
  • 收稿日期:2010-08-28 修回日期:2010-12-18 出版日期:2011-02-19 发布日期:2011-02-19
  • 通讯作者: 杜智，博士，教授，天津市第三中心医院肝胆疾病重点实验室，天津市 300170
  • 作者简介:于美丽，女，1959年生，天津市人，汉族，1982年南开大学毕业，研究员，主要从事生物医用高分子材料及应用研究。 yumeili8@163.com

All-trans retinoic acid-polyanhydride long-term delayed release formulation and feasibility

Yu Mei-li, Du Zhi, Guo Hong-yue, Sun Jin-fang, Du Xue   

  1. Key Laboratory of Hepatobiliary Disease, Tianjin Third Central Hospital, Tianjin  300170, China
  • Received:2010-08-28 Revised:2010-12-18 Online:2011-02-19 Published:2011-02-19
  • Contact: Du Zhi, Doctor, Professor, Key Laboratory of Hepatobiliary Disease, Tianjin Third Central Hospital, Tianjin 300170, China
  • About author:Yu Mei-li, Researcher, Key Laboratory of Hepatobiliary Disease, Tianjin Third Central Hospital, Tianjin 300170, China yumeili8@163.com

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327

被引次数

4

摘要：

背景：如何提高全反式维甲酸疗效、稳定性和降低毒副作用是临床治疗所面临的最大问题。近年来用可生物降解的聚合物为材料，通过乳化包囊等分散技术将药物制备成微粒分散体系，用作缓释、控释注射剂的研究日益增多。
目的：研制全反式维甲酸-聚酸酐长效缓释微球肿瘤治疗剂，观察其体内外全反式维甲酸经时缓释变化规律。
方法：采用乳剂-扩散溶剂挥发法制备全反式维甲酸-聚酸酐长效缓释微球肿瘤治疗剂，扫描电镜检测微球外观及微球粒径，高效液相色谱法检测微球载药量、包封率及体内外释药量。
结果与结论：所制微球治疗剂光滑圆整，大小均一，平均粒径(154.42±26.76) nm，载药率(16.5±1.45)%，包封率(87.84±4.79)%；体外释放实验证明该微球治疗剂可持续释放全反式维甲酸约50 d，将其肌肉注射到大耳白兔体内，可稳定缓释全反式维甲酸近45 d。结果表明该微球治疗剂载药量及包封率均较高，体内外释药平稳并且具有明显的长效缓释作用。

关键词: 全反式维甲酸, 聚酸酐, 微球, 长效缓释, 生物降解材料

Abstract:

BACKGROUND: How to improve the efficacy and stability of all-trans retinoic acid, as well as to reduce side effects are great issues in clinical treatment. In recent years, biodegradable polymers materials are prepared into particle dispersion system by using emulsifying and encapsulation technology, increasing studies investigate its role as a slow and controlled release agent.
OBJECTIVE: To prepare all-trans retinoic acid-polyanhydride (ATRA-PAD) long-term delayed release microspheres therapeutic agent, and to determine slow-release treatment agent ATRA release in vivo and in vitro by the changes of time.
METHODS: A long-acting sustained-release microsphere ATRA-PAD therapeutic agent was established with emulsion/solvent evaporation method, the appearance and microsphere size were detected by using scanning electron microscopy, high performance liquid chromatography was applied to detect the drug loading, encapsulation efficiency, release volume in vivo and in vitro.
RESULTS AND CONCLUSION: The therapeutic microspheres were smooth and had uniform size, the average particle size was (154.42±26.76) nm, drug loading was (16.52±1.45)%, encapsulation efficiency was (87.84±4.79)%; release in vitro experiments indicated that the ATRA sustainable release of the therapeutic agent microsphere was about 50 days, following intramuscular injection into rabbits, ATRA may be stably released for about 45 days. ATRA-PAD microsphere therapeutic agent exhibits high drug loading and encapsulation efficiency, in vivo and in vitro drug release are stable and has obvious long-term sustained action.

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