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香茅醇自乳化递送系统的制备及其体外抗肿瘤活性评价
引用本文:杨佳佳,韦世权,张科,陈妍,姜丰,周雪,肖婷,彭剑青,沈祥春,陶玲.香茅醇自乳化递送系统的制备及其体外抗肿瘤活性评价[J].中草药,2020,51(5):1196-1204.
作者姓名:杨佳佳  韦世权  张科  陈妍  姜丰  周雪  肖婷  彭剑青  沈祥春  陶玲
作者单位:贵州医科大学, 贵州省特色天然药物资源高效利用工程中心(贵州省高等学校天然药物药理与成药性评价特色重点实验室, 贵州医科大学-贵阳市联合重点实验室, 天然药物资源优效利用重点实验室), 药学院, 贵州贵阳 550025,贵州医科大学, 贵州省特色天然药物资源高效利用工程中心(贵州省高等学校天然药物药理与成药性评价特色重点实验室, 贵州医科大学-贵阳市联合重点实验室, 天然药物资源优效利用重点实验室), 药学院, 贵州贵阳 550025,贵州医科大学, 贵州省特色天然药物资源高效利用工程中心(贵州省高等学校天然药物药理与成药性评价特色重点实验室, 贵州医科大学-贵阳市联合重点实验室, 天然药物资源优效利用重点实验室), 药学院, 贵州贵阳 550025;贵州医科大学, 基础医学院现代病原生物学特色重点实验室, 基础医学院寄生虫学教研室, 贵州 贵阳 550025,贵州医科大学, 贵州省特色天然药物资源高效利用工程中心(贵州省高等学校天然药物药理与成药性评价特色重点实验室, 贵州医科大学-贵阳市联合重点实验室, 天然药物资源优效利用重点实验室), 药学院, 贵州贵阳 550025,贵州医科大学, 贵州省特色天然药物资源高效利用工程中心(贵州省高等学校天然药物药理与成药性评价特色重点实验室, 贵州医科大学-贵阳市联合重点实验室, 天然药物资源优效利用重点实验室), 药学院, 贵州贵阳 550025,贵州医科大学, 贵州省特色天然药物资源高效利用工程中心(贵州省高等学校天然药物药理与成药性评价特色重点实验室, 贵州医科大学-贵阳市联合重点实验室, 天然药物资源优效利用重点实验室), 药学院, 贵州贵阳 550025,贵州医科大学, 贵州省特色天然药物资源高效利用工程中心(贵州省高等学校天然药物药理与成药性评价特色重点实验室, 贵州医科大学-贵阳市联合重点实验室, 天然药物资源优效利用重点实验室), 药学院, 贵州贵阳 550025,贵州医科大学, 贵州省特色天然药物资源高效利用工程中心(贵州省高等学校天然药物药理与成药性评价特色重点实验室, 贵州医科大学-贵阳市联合重点实验室, 天然药物资源优效利用重点实验室), 药学院, 贵州贵阳 550025,贵州医科大学, 贵州省特色天然药物资源高效利用工程中心(贵州省高等学校天然药物药理与成药性评价特色重点实验室, 贵州医科大学-贵阳市联合重点实验室, 天然药物资源优效利用重点实验室), 药学院, 贵州贵阳 550025,贵州医科大学, 贵州省特色天然药物资源高效利用工程中心(贵州省高等学校天然药物药理与成药性评价特色重点实验室, 贵州医科大学-贵阳市联合重点实验室, 天然药物资源优效利用重点实验室), 药学院, 贵州贵阳 550025
基金项目:贵阳市科技计划项目(筑科合同[2017]30-25号);贵州省科技创新团队项目(黔科合人才团队[2015]4025号);贵州省高层次创新型人才百层次人才项目(贵州省科技厅黔科合人才[2015]4029号;贵州医科大学药学国际科技合作基地(黔科合平台人才[2017]5802)
摘    要:目的考察香茅醇(citronellol,CT)对人喉癌上皮细胞HEp-2和人乳腺癌细胞MCF-7增殖能力的影响,并制备CT自乳化递送系统(self-emulsified drug delivery system,SMs),对HEp-2体外抗肿瘤活性和细胞摄取能力进行评价。方法采用MTT法考察CT对HEp-2和MCF-7细胞增殖能力的影响;通过伪三元相图法优化香茅醇自乳化递送系统(CT-SMs)处方,进行外观形态、粒径和Zeta电位表征。采用MTT法检测CT-SMs对HEp-2细胞增殖能力的影响;荧光倒置显微镜定性和流式细胞仪定量考察HEp-2细胞对CT-SMs的摄取情况。结果经一定质量浓度CT处理后,MCF-7细胞增殖未受影响,差异无统计学意义(与对照组相比,P0.05),而HEp-2细胞的增殖能力受到明显抑制(与对照组相比,P0.05),呈剂量-时间依赖性;CT-SMs最佳处方是K_m(乳化剂与助乳化剂比例)为Kolliphor~?HS15-无水乙醇7∶3,CT-Km为3∶7。制备的微乳平均粒径为(354.0±9.5)nm,外观圆整呈类球形,分布均匀,Zeta电位为(-13.4±0.3)m V。细胞摄取实验结果表明,相同质量浓度的CT-SMs和CT处理HEp-2细胞后,CT-SMs较CT摄取量更多,分别为545.70±11.56、230.00±17.76。结论。采用滴加水法成功制备了CT-SMs,其处方工艺可行,制得的自微乳质量稳定可控。CT-SMs可明显抑制HEp-2细胞的增殖。

关 键 词:香茅醇|自乳化递送系统|抗肿瘤|人喉癌上皮细胞|乳腺癌细胞|细胞摄取|细胞增殖|MTT法|伪三元相图
收稿时间:2019/10/10 0:00:00

Preparation of citronellol self-emulsifying delivery system and evaluation of its in vitro antitumor activity
YANG Jia-ji,WEI Shi-quan,ZHANG Ke,CHEN Yan,JIANG Feng,ZHOU Xue,XIAO Ting,PENG Jian-qing,SHEN Xiang-chun and TAO Ling.Preparation of citronellol self-emulsifying delivery system and evaluation of its in vitro antitumor activity[J].Chinese Traditional and Herbal Drugs,2020,51(5):1196-1204.
Authors:YANG Jia-ji  WEI Shi-quan  ZHANG Ke  CHEN Yan  JIANG Feng  ZHOU Xue  XIAO Ting  PENG Jian-qing  SHEN Xiang-chun and TAO Ling
Institution:Guizhou Province Specialized Natural Medicine Resource Efficient Utilization Engineering Center(Key Laboratory of Pharmacology and Pharmacological Evaluation of Natural Medicines in Guizhou Higher Education Institutions, Guizhou Medical University-Guiyang Joint Key Laboratory, Key Laboratory of Utilization of Natural Medicine Resources) College of Pharmacy, Guizhou Medical University, Guiyang 550025, China,Guizhou Province Specialized Natural Medicine Resource Efficient Utilization Engineering Center(Key Laboratory of Pharmacology and Pharmacological Evaluation of Natural Medicines in Guizhou Higher Education Institutions, Guizhou Medical University-Guiyang Joint Key Laboratory, Key Laboratory of Utilization of Natural Medicine Resources) College of Pharmacy, Guizhou Medical University, Guiyang 550025, China,Guizhou Province Specialized Natural Medicine Resource Efficient Utilization Engineering Center(Key Laboratory of Pharmacology and Pharmacological Evaluation of Natural Medicines in Guizhou Higher Education Institutions, Guizhou Medical University-Guiyang Joint Key Laboratory, Key Laboratory of Utilization of Natural Medicine Resources) College of Pharmacy, Guizhou Medical University, Guiyang 550025, China;Key Laboratory of Modern Pathogenic Biology, Department of Parasitology, School of Basic Medical Sciences, Guizhou Medical University, Guiyang 550025, China,Guizhou Province Specialized Natural Medicine Resource Efficient Utilization Engineering Center(Key Laboratory of Pharmacology and Pharmacological Evaluation of Natural Medicines in Guizhou Higher Education Institutions, Guizhou Medical University-Guiyang Joint Key Laboratory, Key Laboratory of Utilization of Natural Medicine Resources) College of Pharmacy, Guizhou Medical University, Guiyang 550025, China,Guizhou Province Specialized Natural Medicine Resource Efficient Utilization Engineering Center(Key Laboratory of Pharmacology and Pharmacological Evaluation of Natural Medicines in Guizhou Higher Education Institutions, Guizhou Medical University-Guiyang Joint Key Laboratory, Key Laboratory of Utilization of Natural Medicine Resources) College of Pharmacy, Guizhou Medical University, Guiyang 550025, China,Guizhou Province Specialized Natural Medicine Resource Efficient Utilization Engineering Center(Key Laboratory of Pharmacology and Pharmacological Evaluation of Natural Medicines in Guizhou Higher Education Institutions, Guizhou Medical University-Guiyang Joint Key Laboratory, Key Laboratory of Utilization of Natural Medicine Resources) College of Pharmacy, Guizhou Medical University, Guiyang 550025, China,Guizhou Province Specialized Natural Medicine Resource Efficient Utilization Engineering Center(Key Laboratory of Pharmacology and Pharmacological Evaluation of Natural Medicines in Guizhou Higher Education Institutions, Guizhou Medical University-Guiyang Joint Key Laboratory, Key Laboratory of Utilization of Natural Medicine Resources) College of Pharmacy, Guizhou Medical University, Guiyang 550025, China,Guizhou Province Specialized Natural Medicine Resource Efficient Utilization Engineering Center(Key Laboratory of Pharmacology and Pharmacological Evaluation of Natural Medicines in Guizhou Higher Education Institutions, Guizhou Medical University-Guiyang Joint Key Laboratory, Key Laboratory of Utilization of Natural Medicine Resources) College of Pharmacy, Guizhou Medical University, Guiyang 550025, China,Guizhou Province Specialized Natural Medicine Resource Efficient Utilization Engineering Center(Key Laboratory of Pharmacology and Pharmacological Evaluation of Natural Medicines in Guizhou Higher Education Institutions, Guizhou Medical University-Guiyang Joint Key Laboratory, Key Laboratory of Utilization of Natural Medicine Resources) College of Pharmacy, Guizhou Medical University, Guiyang 550025, China and Guizhou Province Specialized Natural Medicine Resource Efficient Utilization Engineering Center(Key Laboratory of Pharmacology and Pharmacological Evaluation of Natural Medicines in Guizhou Higher Education Institutions, Guizhou Medical University-Guiyang Joint Key Laboratory, Key Laboratory of Utilization of Natural Medicine Resources) College of Pharmacy, Guizhou Medical University, Guiyang 550025, China
Abstract:
Keywords:citronellol|self-emulsifying delivery system|antitumor activity|laryngeal cancer cells|breast cancer cells|cellular uptake|cell proliferation|MTT assay|pseudo-ternary phase diagram
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