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REN Jing,ZHANG Danshen,HOU Wenshu,WU Chunyang,MA Jiacheng.Preparation and characterization of curcumin long-circulating liposomes[J].Journal of Hebei University of Science and Technology,2018,39(6):532-539
姜黄素长循环脂质体的制备及表征
Preparation and characterization of curcumin long-circulating liposomes
Received:September 07, 2018  Revised:October 08, 2018
DOI:10.7535/hbkd.2018yx06008
中文关键词:  中药药剂学  姜黄素  长循环脂质体  包封率  体外释放
英文关键词:pharmacy of Chinese materia medica  curcumin(Cur)  long circulating liposomes  encapsulation rate  in vitro release
基金项目:河北省自然科学基金面上项目(H2016208058); 河北省自然科学基金(H2016208059); 河北省高等学校科学技术研究项目(ZD2016009)
Author NameAffiliationE-mail
REN Jing School of Chemical and Pharmaceutical Engineering Hebei University of Science and Technology Shijiazhuang  
ZHANG Danshen School of Chemical and Pharmaceutical Engineering Hebei University of Science and Technology Shijiazhuang zhangds2011@126.com 
HOU Wenshu School of Pharmacy Hebei North University Zhangjiakou  
WU Chunyang School of Pharmacy Hebei North University Zhangjiakou  
MA Jiacheng School of Pharmacy Hebei North University Zhangjiakou  
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中文摘要:
      为了改善姜黄素长循环脂质体(Cur-LCL)的稳定性,延长药物在体内的循环时间,对现有姜黄素脂质体(Cur-Lips)和姜黄素长循环脂质体的制备方法进行了优化。使用乙醇注入法制备Cur-Lips,用后插法将DSPE-PEG2000插入Cur-Lips中制成Cur-LCL。结果表明:Cur-LCL外观为圆形囊泡状球体,平均包封率为(88.91±0.94)%,4 ℃存放15 d包封率没有明显变化,平均渗漏率为2.4%,具有较好的稳定性;Cur-LCL平均粒径为(118.4±3.2)nm(n=3),呈单峰分布,平均电位为(-12.9±0.32)mV(n=3);以溶解度为标准对溶出介质进行筛选,选择以1% Tween 80的生理盐水为体外释放试验的溶出介质,Cur原料药12 h基本释放完全,Cur-Lips在36 h基本释放完全,累计释放率为92.67%,Cur-LCL在72 h基本释放完全,累计释放率为91.36%。Cur-LCL具有明显的缓释性,可以延长药物在血液中的循环时间,达到长循环的效果。
英文摘要:
      In order to improve the stability of Cur-LCL and extend the circulation time of the drug in the body, the existing methods of preparing curcumin liposomes (Cur-Lips) and curcumin long-circulating liposomes (Cur-LCL) are optimized. Cur-Lips are prepared by ethanol injection method, and the Cur-LCL is prepared by inserting DSPE-PEG2000 into Cur-Lips by post-insertion. The results show the appearance is a circular vesicular sphere, and the average encapsulation efficiency is (88.91±0.94)%, which stays unchanged at 4 ℃ for 15 days; the average leakage rate is 2.4%, which has good stability; the average particle size is (118.4±3.2) nm (n=3), showing a single peak distribution, and the average potential is (-12.9±0.32) mV (n=3); the dissolution medium is selected according to the solubility standard, and the physiological solution of 1% Tween 80 is selected as the dissolution medium for the in vitro release experiment. Cur APIs are almost completely released at 12 h while Cur-Lips are almost completely released at 36 h, and the cumulative release rate is 92.67%. Cur-LCL is almost completely released at 72 h, and the cumulative release rate is 91.36%. Cur-LCL has obvious function in slowing the release process, which could prolong the circulation time of the drug in the blood and achieve long-circulation effects.
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