中国组织工程研究

中国组织工程研究 ›› 2022, Vol. 26 ›› Issue (28): 4489-4493.doi: 10.12307/2022.303

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

姜黄素缓释微球的制备及体外释放

李希凯1，孟永春2，付  丽1，刘  卿1，王  笑1，谷成旭1，黄  飞1   

  1. 1滨州医学院基础医学院解剖学教研室，山东省烟台市   264000；2滨州医学院康复医学院，山东省烟台市   264000
  • 收稿日期:2020-12-18 接受日期:2021-01-27 出版日期:2022-10-08 发布日期:2022-03-23
  • 通讯作者: 黄飞，博士，教授，滨州医学院基础医学院解剖学教研室，山东省烟台市 264000
  • 作者简介:李希凯，男，1992年生，山东省烟台市人，汉族，滨州医学院在读硕士，主要从事脊髓损伤修复研究。
  • 基金资助:
    山东省自然科学基金(ZR2017MC052)，项目负责人：黄飞；国家自然科学基金(81870985)，项目负责人：黄飞

Preparation and in vitro release of curcumin sustained-release microspheres

Li Xikai1, Meng Yongchun2, Fu Li1, Liu Qing1, Wang Xiao1, Gu Chengxu1, Huang Fei1   

  1. 1Department of Anatomy, Basic Medical College, Binzhou Medical University, Yantai 264000, Shandong Province, China; 2School of Rehabilitation Medicine, Binzhou Medical University, Yantai 264000, Shandong Province, China
  • Received:2020-12-18 Accepted:2021-01-27 Online:2022-10-08 Published:2022-03-23
  • Contact: Huang Fei, PhD, Professor, Department of Anatomy, Basic Medical College, Binzhou Medical University, Yantai 264000, Shandong Province, China
  • About author:Li Xikai, Master candidate, Department of Anatomy, Basic Medical College, Binzhou Medical University, Yantai 264000, Shandong Province, China
  • Supported by:
    the Natural Science Foundation of Shandong Province, No. ZR2017MC052 (to HF); the National Natural Science Foundation of China, No. 81870985 (to HF)

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摘要：

文题释义：
姜黄素：是姜黄的主要活性成分，呈黄色，从干姜黄根茎粉中提取，具有抗氧化剂、抗炎、抗纤维化和抗肿瘤等特性，这些特性可由转录因子、生长因子、受体、细胞因子等多种分子靶点介导。大量证据表明，姜黄素对中枢神经系统具有神经保护作用。
一级释放：药物释放速率不随时间变化而改变，药物在释放周期内速率保持恒比释放。
零级释放：药物释放速率不随时间变化而改变，药物在释放周期内速率保持恒量释放。

背景：姜黄素具有抑制炎症、促进轴突生长等作用，但存在半衰期短、清除速度快等问题。
目的：制备姜黄素缓释微球，以达到缓慢持续释放姜黄素的效果。
方法：以聚乳酸-羟基乙酸共聚物为原料，采用O/W乳化挥发法合成合成姜黄素缓释微球，预设载药率分别为10%和20%，设为1、2号微球；以左旋聚乳酸-聚己内酯共聚物聚合物为原料，采用O/W乳化挥发法合成合成姜黄素缓释微球，预设载药率分别为10%和20%，设为3、4号微球，扫描电镜观察微球的表面形态特征，高效液相色谱检测微球的载药量和包封率。将4组微球浸泡在含有1%十二烷基硫酸钠的PBS释放外液中，模拟生理环境检测姜黄素微球的缓释情况。
结果与结论：①扫描电镜显示，3、4号姜黄素微球的粒径、形态均优于1、2号姜黄素微球。②3号微球的包封率高于其他3组微球(P  < 0.05，P  < 0.01)，1、2、4号微球的包封率比较差异无显著性意义(P > 0.05)。③2、3、4号微球的载药率高于1号微球(P < 0.01)，2、4号微球的载药率高于3号微球(P < 0.01)。④3号姜黄素缓释微球的体外释放可持续14 d，其余3种微球的体外释放可持续21 d，1、3号微球的药物累积释放率高于2、4号微球，3号微球的姜黄素释放浓度高于1号微球。⑤结果表明，以左旋聚乳酸-聚己内酯共聚物为原料合成的预设载药率10%的姜黄素缓释微球，缓释效果最接近零级释放要求。

https://orcid.org/0000-0002-2827-4041 (李希凯) 

中国组织工程研究杂志出版内容重点：生物材料；骨生物材料；口腔生物材料；纳米材料；缓释材料；材料相容性；组织工程

关键词: 姜黄素, 缓释微球, 聚乳酸, 羟基乙酸共聚物, 左旋聚乳酸, 聚己内酯, 体外释放

Abstract: BACKGROUND: Curcumin can inhibit inflammation and promote axonal growth, but it has a short half-life and a fast clearance rate.  
OBJECTIVE:  To prepare curcumin sustained-release microspheres to release curcumin slowly and continuously.
METHODS:  Curcumin sustained-release microspheres were synthesized by O/W emulsification volatilization method using polylactic acid-glycolic acid copolymer as raw material. The preset drug loading rates were 10% and 20%, respectively, and set as No. 1 and No. 2 microspheres. The curcumin sustained release microspheres were synthesized by O/W emulsification volatilization method using L-lactic acid-polycaprolactone copolymer as raw material. The preset drug loading rates were 10% and 20%, respectively, and the microspheres were set as No. 3 and No. 4. The surface morphology of the microspheres was observed by scanning electron microscopy, and the drug loading and encapsulation efficiency of the microspheres were determined by high performance liquid chromatography. Four groups of microspheres were immersed in PBS release solution containing 1% sodium dodecyl sulfate, and the sustained release of curcumin microspheres was detected under simulated physiological environment.    
RESULTS AND CONCLUSION: (1) Scanning electron microscopy showed that the particle size and morphology of No. 3 and No. 4 curcumin microspheres were better than those of No. 1 and No. 2 curcumin microspheres. (2) The encapsulation rate of No. 3 microspheres was higher than that of the other three groups (P < 0.05, P < 0.01), and there was no significant difference in the encapsulation rate of No. 1, 2 and 4 microspheres (P > 0.05). (3) The drug loading rates of No. 2, 3 and 4 microspheres were higher than that of No. 1 microsphere (P < 0.01), and the drug loading rates of No. 2 and 4 microspheres were higher than that of No. 3 microsphere (P < 0.01). (4) The in vitro release of No. 3 curcumin sustained-release microspheres lasted for 14 days, and the release of the other three kinds of microspheres lasted for 21 days. The cumulative release rate of No. 1 and No. 3 was higher than that of No. 2 and No. 4, and the curcumin release concentration of No. 3 was higher than that of No. 1. (5) The results showed that slow-release effect of the curcumin sustained-release microspheres with a preset loading rate of 10% prepared by L-lactic acid-polycaprolactone copolymer best meets the Zero order release requirements.

Key words: curcumin, curcumin sustained-release microspheres, polylactic acid, glycolic acid copolymer, L-polylactic acid, polycaprolactone, in vitro release

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