姜黄素长循环脂质体的制备及表征
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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)


Preparation and characterization of curcumin long-circulating liposomes
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    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。

    Abstract:

    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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任 婧,张丹参,侯文书,武春阳,马佳呈.姜黄素长循环脂质体的制备及表征[J].河北科技大学学报,2018,39(6):532-539

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  • 收稿日期:2018-09-07
  • 最后修改日期:2018-10-08
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  • 在线发布日期: 2018-12-26
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