藤黄有效成分的纳米囊制备及其抗糖尿病活性评价
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篇名: 藤黄有效成分的纳米囊制备及其抗糖尿病活性评价
TITLE: Preparation of nanocapsules of active ingredients of Garcinia hanburyi and evaluation of their antidiabetic activity
摘要: 目的 制备藤黄酸(GA)、新藤黄酸(NGA)的纳米囊(GA-LNCs、NGA-LNCs),并进行其抗糖尿病活性评价。方法以水为水相、中链甘油三酯为油相、聚乙二醇单硬脂酸酯为表面活性剂,采用相转换法制备GA-LNCs、NGA-LNCs。以包封率和载药量为指标,利用单纯型网格设计法优化上述2种纳米囊的处方工艺,并对其理化性质进行考察。建立糖尿病小鼠模型,灌胃给予GA-LNCs、NGA-LNCs(剂量分别为1.92、2.42mg/kg),每天1次,连续给药6周,检测小鼠空腹血糖值和血清中超氧化物歧化酶(SOD)、谷胱甘肽过氧化物酶(GSH-Px)活性以及丙二醛(MDA)、总胆固醇(TC)、三酰甘油(TG)、高密度脂蛋白胆固醇(HDL-C)、低密度脂蛋白胆固醇(LDL-C)含量。结果这2种纳米囊的最优处方均为60%水、10%中链甘油三酯、30%聚乙二醇单硬脂酸酯(三者总量固定为2g)以及35mgGA或NGA。以最优处方制得的GA-LNCs、NGA-LNCs的包封率分别为(92.01±0.68)%、(93.12±2.11)%,载药量分别为(0.99±0.21)%、(1.21±0.22)%;两者均为黄色均一透明液体,无沉淀,微观形态均为类球形,且具有明显的壳膜结构,粒径分别为(28.11±9.76)、(22.06±6.84)nm,Zeta电位分别为(-4.09±1.00)、(-17.40±1.32)mV,多分散系数分别为0.93±0.06、0.74±0.12。动物实验结果显示,GA-LNCs、NGA-LNCs均可显著升高模型小鼠血清中SOD、GSH-Px活性和HDL-C含量(P<0.05或P<0.01),显著降低模型小鼠空腹血糖值和血清中MDA、TC、TG、LDL-C含量(P<0.05或P<0.01)。结论本研究制得的GA-LNCs、NGA-LNCs理化性质良好,且具有良好的抗糖尿病活性。
ABSTRACT: OBJECTIVE To prepare Gambogic acid (GA) nanocapsules (GA-LNCs) and Neogambogic acid (NGA) nanocapsules(NGA-LNCs),and to evaluate their antidiabetic activities. METHODS Using water as the aqueous phase ,medium- chain triglyceride as the oil phase and polyethylene glycol monostearate as the surfactant ,GA-LNCs and NGA-LNCs were prepared by phase inversion method. Using entrapment efficiency and drug-loading amount as index ,the formulation technologies of above 2 nanocapsules were optimized by simplex lattice design. Its physical and chemical properties were investigated. The diabetic mice model was established. GA-LNCs and NGA-LNCs (1.92 and 2.42 mg/kg respectively )were given intragastrically ,once a day ,for consecutive 6 weeks. The fasting blood glucose of mice ,the activities of superoxide dismutase (SOD)and glutathione peroxidase (GSH-Px),the contents of malondialdehyde (MDA),total cholesterol (TC),triglyceride (TG),high-density lipoprotein cholesterol(HDL-C)and low-density lipoprotein cholesterol (LDL-C)were all detected. RESULTS The optimal formulation of 2 kinds of nanocapsules included 60% water,10% medium-chain triglyceride ,30% polyethylene glycol monostearate (total amount of the three was 2 g)and 35 mg GA or NGA . The encapsulation efficiencies of GA-LNCs and NGA-LNC obtained by the optimal formulation were (92.01±0.68)% and(93.12±2.11)%;the drug-loading amount were (0.99±0.21)% and(1.21±0.22)%, respectively. GA-LNCs and NGA-LNCs were yellow ,homogeneous and transparent liquid without precipitation. They were spherical in microscopic shape , and had obvious shell- Δ 基金项目:吉林省科技发展计划项目(No.20200404090YY);吉 membrane structure. The particle sizes were (28.11 ± 9.76) 林省教育厅科学技术研究项目(No.JJKH20210372KJ) *硕士研究生 。研究方向 :植物药 。E-mail:zhanhe0108@163. and(22.06±6.84)nm;Zeta potential were (-4.09±1.00) com and(-17.40±1.32)mV,and polydispersity were 0.93±0.06 # 通信作者:讲师,博士。研究方向:中药有效成分治疗疾病的作 and 0.74±0.12. The results of animal experiments showed that 用机制。E-mail:chenweijia_jlau@163.com both GA-LNCs and NGA-LNCs could sig nificantly increase 中国药房 2022年第33卷第9期 China Pharmacy 2022Vol. 33 No. 9 ·1075· the activities of SOD and GSH-Px and the seru m content of HDL-C (P<0.05 or P<0.01)in model mice ,and significantly decreased the fasting blood glucose and the serum contents of MDA , TC, TG and LDL-C (P<0.05 or P<0.01). CONCLUSIONS GA-LNCs,NGA-LNCs prepared in this study are good in physical and chemical properties and have good anti-diabetes activity.
期刊: 2022年第33卷第09期
作者: 战鹤,韩璐,何忠梅,时坤,赵岩,宗颖,陈维佳,杜锐
AUTHORS: ZHAN He,HAN Lu,HE Zhongmei ,SHI Kun,ZHAO Yan,ZONG Ying,CHEN Weijia ,DU Rui
关键字: 藤黄酸;新藤黄酸;纳米囊;糖尿病;制备
KEYWORDS: gambogic acid ;neogambogic acid ;nanocapsules;diabetes;preparation
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