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、2.42 mg/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2 g)以及35 mg GA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。
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,mediumchain 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 shellmembrane structure.The particle sizes were(28.11±9.76)and(22.06±6.84)nm;Zeta potential were(-4.09±1.00)and(-17.40±1.32)mV,and polydispersity were 0.93±0.06 and 0.74±0.12.The results of animal experiments showed that both GA-LNCs and NGA-LNCs could significantly increase the activities of SOD and GSH-Px and the serum 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)
作者
战鹤
韩璐
何忠梅
时坤
赵岩
宗颖
陈维佳
杜锐
ZHAN He;HAN Lu;HE Zhongmei;SHI Kun;ZHAO Yan;ZONG Ying;CHEN Weijia;DU Rui(College of Chinese Medicinal Materials,Jilin Agricultural University,Changchun 130118,China;Key Laboratory of Animal Production,Product Quality and Security,Ministry of Education of China,Changchun 130118,China;Jilin Provincial Engineering Research Center for Efficient Breeding and Product Development of Sika Deer of China,Changchun 130118,China)
出处
《中国药房》
CAS
北大核心
2022年第9期1075-1081,共7页
China Pharmacy
基金
吉林省科技发展计划项目(No.20200404090YY)
吉林省教育厅科学技术研究项目(No.JJKH20210372KJ)。
关键词
藤黄酸
新藤黄酸
纳米囊
糖尿病
制备
gambogic acid
neogambogic acid
nanocapsules
diabetes
preparation
