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

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。

Preparation and physicochemical characterization of folic acid modified nanostructured lipid carrier loaded with tanshinone ⅡA

Objective] The nanostructured lipid carrier(NLC) loaded with tanshinone Ⅱ A 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.