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叶酸修饰载丹参酮ⅡA纳米结构脂质载体的制备及其理化表征
刘静静1,2, 李新悦1,2, 吴玉梅1,2, 马丽1,2, 张兵1,2, 刘志东1,2, 李佳玮1,2
1.天津中医药大学, 现代中药发现与制剂技术教育部工程中心, 天津 301617;2.天津中医药大学, 天津市现代中药重点实验室-省部共建国家重点实验室培育基地, 天津 301617
摘要:
[目的] 制备载丹参酮ⅡA纳米结构脂质载体,将含有叶酸的PEG链配体修饰于制剂表面获得叶酸修饰载丹参酮ⅡA纳米结构脂质载体(FA-TanⅡA-NLC),使其具有肿瘤靶向作用,并对制剂进行理化表征。[方法] 采用乳化蒸发-低温固化法制备制剂,以粒径、电位和包封率等为指标对制剂进行初步评价,采用透射电子显微镜(TEM)、差示扫描量热法(DSC)和X射线衍射法(XRD)对制剂进行进一步的表征。[结果] 制备的叶酸修饰载丹参酮ⅡA纳米结构脂质载体(FA-TanⅡA-NLC)粒径为(19.14±0.43)nm,PDI为0.424±0.01,电位为(-11.67±0.25)mV,DSC以及XRD结果均表明丹参酮ⅡA以无定型形式被包载于纳米结构脂质载体中。[结论] 本研究制得的FA-TanⅡA-NLC粒径分布均一,体系稳定,包封率高。
关键词:  丹参酮ⅡA  纳米结构脂质载体  叶酸
DOI:10.11656/j.issn.1673-9043.2020.01.21
分类号:R283
基金项目:
Preparation and physicochemical characterization of folic acid modified nanostructured lipid carrier loaded with tanshinone ⅡA
LIU Jingjing1,2, LI Xinyue1,2, WU Yumei1,2, MA Li1,2, ZHANG Bing1,2, LIU Zhidong1,2, LI Jiawei1,2
1.Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China;2.Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-Established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Abstract:
[Objective] The nanostructured lipid carrier (NLC) loaded with tanshinone ⅡA was prepared and modified by inserting the DSPE-PEG-FA on its surface,and the physicochemical characterizations of the NLC were investigated.[Methods] The FA-TanⅡA-NLC was prepared by emulsification-evaporation technique. The particle size,zeta potential and encapsulation efficiency were used to preliminarily evaluate the NLC,which was further characterized by TEM,DSC and XRD.[Results] The particle diameter of FA-Tan ⅡA-NLC was of (19.14±0.43) nm, PDI was 0.424±0.01,and the zeta potential was of (-11.67±0.25) mV. The encapsulation efficiency was 99%. The results of DSC and XRD indicated that tanshinone ⅡA was encapsulated in the nanostructured lipid carrier in an amorphous form.[Conclusion] The FA-TanIIA-NLC prepared in this experiment had uniform particle size distribution,stable potential and high encapsulation efficiency.
Key words:  tanshinone ⅡA  nanostructure lipid carrier  folic acid
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