藤黄酸纳米结构脂质载体的制备及抗肿瘤作用初步评价

The preparation and preliminary evaluation of anti-tumor effect of Gambogic acid nanostructure lipid carrier

[目的]制备抗肿瘤药物藤黄酸(GA)纳米结构脂质载体(GA-NLC),考察其理化性质,并对其抗肿瘤作用进行初步评价。[方法]采用乳化-固化法制备,以粒径、Zeta电位、包封率为评价指标考察其理化性质,并用差示扫描量热法(DSC)进行验证。采用CCK-8法测定GA-NLC对人乳腺癌细胞MDA-MB-231的抑制作用。[结果]制备的GANLC粒径分布在20 nm左右,Zeta电位为-(5.86±0.64)mV、包封率为(99.46±0.23)%。DSC结果表明GA以无定型的形式存在于藤黄酸纳米结构脂质载体中。[结论]通过乳化-固化法制备出的GA-NLC,粒径较小、分布均匀,包封率高,与GA溶液相比,GA-NLC具有更强的抗肿瘤活性。

Objective] To prepare the nanostructure lipid carriers （NLC） incorporated gambogic acid （GA） , investigate its physical and chemical properties and evaluate the anti-tumor effect preliminarily. [Methods] Emulsification-evaporation was used to prepare the nanoparticles. The particle size, Zeta potential, encapsulation efficiency were selected as the evaluation indexs to appraise the physical and chemical properties and process validation was implemented by using differential scanning calorimetry （DSC）. The CCK-8 assay was used to measure human breast cancer cells MDA-MB-231 cell growth repression rate. [Results] The GA-NLC was about 20 nm in diame-ter. Zeta potential was-（5.86＆#177;0.64） mV. The encapsulation efficiency was （99.46＆#177;0.23）%. DSC results showed that GA exists in gambog-ic acid nanostructure lipid carrier in the form of amorphous. [Conclusion] The GA-NLC prepared by emulsification-evaporation was characterized of smaller particle size, uniform distribution and high encapsulation efficiency. Compared with GA solution, GA-NLC has a significant antitumor activity.