细胞穿膜肽PFV修饰紫杉醇/青蒿琥酯共载靶向胶束的制备及体外抗肿瘤作用研究-中国药房

细胞穿膜肽PFV修饰紫杉醇/青蒿琥酯共载靶向胶束的制备及体外抗肿瘤作用研究

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篇名：	细胞穿膜肽PFV修饰紫杉醇/青蒿琥酯共载靶向胶束的制备及体外抗肿瘤作用研究
TITLE：	Study on Preparation and in vitro Anticancer Activity of PFV-modified Paclitaxel/artesunate Co-loaded Targeting Micelles
摘要：	目的：制备细胞穿膜肽PFV修饰紫杉醇（PTX）/青蒿琥酯（ART）共载靶向胶束，并考察其体外抗肿瘤活性。方法：按前期优化的工艺，采用薄膜水化法制备PFV修饰PTX/ART共载靶向胶束，并对其进行表征。以空白胶束作为空白对照，采用磺基罗丹明B法评价PTX胶束、ART胶束、PTX/ART胶束以及PFV修饰PTX/ART共载靶向胶束对人胃癌BGC-823细胞的毒性；以香豆素作为荧光探针取代PTX，制成相应的不同胶束，采用流式细胞仪和荧光显微镜测定和观察BGC-823细胞对各胶束的摄取情况和靶向性；并通过Transwell小室法考察PTX胶束、ART胶束、PTX/ART胶束以及PFV修饰PTX/ART共载靶向胶束对BGC-823细胞侵袭的影响。结果：PFV修饰PTX/ART共载靶向胶束的平均粒径为（51.30±3.95）nm，分散系数为0.19±0.01，Zeta电位为（0.21±0.02）mV，PTX、ART的包封率均高于90％，形态呈圆球形。空白胶束对BGC-823细胞无明显毒性，PTX胶束、PTX/ART胶束以及PFV修饰PTX/ART共载靶向胶束对BGC-823细胞的半数抑制浓度分别为（3.09±0.22）、（1.93±0.24）、（1.11±0.15）μmol/L；不同胶束在BGC-823细胞核中的分布数量排序依次为PFV修饰香豆素/ART胶束＞香豆素/ART胶束＞香豆素胶束＞空白对照，抑制细胞侵袭作用的大小依次为PFV修饰PTX/ART共载靶向胶束＞PTX/ART胶束＞ART胶束＞PTX胶束＞空白对照。结论：制备的PFV修饰PTX/ART共载靶向胶束符合《中国药典》要求；其对BGC-823细胞具有较强的细胞毒性，可提高药物的靶向性和细胞对药物的摄取能力，并能抑制肿瘤细胞的侵袭和转移。
ABSTRACT：	OBJECTIVE：To prepare cell penetrating peptide PFV-modified paclitaxel （PTX）/artesunate（ART）co-loaded targeting micelles ，and to investigate in vitro anti-tumor activity. METHODS ：According to optimal technology ，PFV-modified PTX/ ART co-loaded targeting micelles were prepared by membrane hydration method ，and were characterized. Using blank micelle as blank control ，sulforhodamine B （SRB）method was used to evaluate the toxicity of PTX micelles ，ART micelles ，PTX/ART micelles and PFV-modified PTX/ART co-loaded targeting micelles to human gastric cancer BGC- 823 cells. The coumarin was used as fluorescent probe replacing PTX to prepare corresponding micelles. Then ，the uptake of BGC- 823 cells to corresponding micelles and targeting effect were observed and determined by flow cytometry and fluorescence microscope. The effects of PTX micelles ， ART micelles ，PTX/ART micelles and PFV-modified PTX/ART co-loaded targeting micelles on the invasion of BGC- 823 cells were investigated by Transwell chamber method. RESULTS ：Average particle size of PFV-modified PTX/ART co-loaded targeting micelles was （51.30±3.95）nm；PDI was 0.19±0.01，and Zeta potential was （0.21±0.02）mV. The encapsulation efficiency of PTX and ART were higher than 90％. The shape of micelles were spherical. The blank micelles had no obvious toxicity to BGC-823 cells. The IC 50 value of PTX micelles ，PTX/ART micelles and PFV-modified PTX/ART co-loaded targeting micelles to BGC-823 cells were （3.09±0.22），（1.93±0.24），（1.11±0.15）μmol/L，respectively. The distribution amount of different micelles in BGC- 823 cell nucleus in the descending order were PFV-modified coumarin/ART micelles ＞coumarin/ART micelles ＞coumarin micelles＞blank control. The order of inhibitory effect was PFV-modified PTX/ART co-loaded targeting micelles ＞PTX/ART micelles＞ART micelles ＞PTX micelles ＞blank control. CONCLUSIONS： Prepared PFV-modified PTX/ART No.81874347） co-loaded targeting micelles are in line with the quality of 1915286446@qq.com Chinese Pharmacopoeia . It shows strong cytotoxicity to BGC-823 cells，can improve the drug targeting and the cell uptake，and inhibit the inv asion and metastasis of BGC- 823 cells.
期刊：	2020年第31卷第21期
作者：	王为，李学涛，孔亮，姜爽，罗一夫，王晓波
AUTHORS：	WANG Wei，LI Xuetao ，KONG Liang，JIANG Shuang ，LUO Yifu，WANG Xiaobo
关键字：	细胞穿膜肽；紫杉醇；青蒿琥酯；胶束；人胃癌BGC-823细胞；靶向作用；抗肿瘤作用
KEYWORDS：	Cell-penetrating peptide ；Paclitaxel；Micelles；Artesunate；Human gastric cancer BGC- 823 cells；Targeting effects；
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