三七总皂苷心肌靶向脂质体的处方、制备工艺优化及质量评价  

Prescription,preparation process optimization and quality evaluation of myocardium-target⁃ing liposomes of panax notoginseng saponins

作　　者：冯慧 谢佳秀 韦柱梅 黄玉鹏 黄建春[1] Feng Hui;Xie Jiaxiu;Wei Zhumei;Huang Yupeng;Huang Jianchun(Pharmaceutical College,Guangxi Medical University,Nanning 530021,China)

机构地区：[1]广西医科大学药学院,南宁530021

出　　处：《广西医科大学学报》2023年第6期1062-1068,共7页Journal of Guangxi Medical University

基　　金：国家自然科学基金资助项目(No.81560587);广西自然科学基金资助项目(No.2018GXNSFAA050073);广西壮族自治区大学生创新创业训练计划项目(No.202010598148)。

摘　　要：目的:优化三七总皂苷心肌靶向脂质体的处方和制备工艺,并对其进行质量评价。方法:采用薄膜分散超声法制备三七总皂苷普通脂质体(L-PNS),通过单因素实验和响应面设计实验优化L-PNS处方,根据最优处方制备由艾司洛尔类似物(PAC)修饰的三七总皂苷心肌靶向脂质体(PAC-L-PNS),并对其进行表征研究、储存稳定性及体外释药特性考察。结果:L-PNS的最优处方与制备工艺为:磷脂与胆固醇的质量比为9∶1,药物与磷脂的比例1∶20,超声功率为63 W,超声时间为10 min,水化时间为15 min,药物浓度为1 mg/mL。在最优处方基础上制备的PAC-L-PNS粒径为(222.70±2.55)nm,Zeta电位为(+32.73±0.25)mV,包封率和载药量分别为64.62%、11.52%;稳定性实验结果显示,L-PNS和PAC-L-PNS在48 h内的渗漏率均低于30%,没有出现突释现象,稳定性良好;体外释药结果显示,L-PNS和PAC-L-PNS 72 h的累积释放率分别为35.88%、32.86%,均平稳释放,无明显的突释行为,具有缓控释作用。结论:根据最优处方和制备工艺,采用薄膜分散超声法制得的PAC-L-PNS粒径分布均匀、表面带正电荷,避光储存稳定性良好,体外释放缓慢。Objective:To optimize the prescription and preparation process of myocardium-targeting liposomes of panax notoginseng saponins and evaluate its quality.Methods:The common liposomes of panax notoginseng saponins(L-PNS)were prepared by thin-film dispersion plus ultrasonic method.Single-factor experiment and response surface design methodology were carried out to optimize the prescription of L-PNS.Then L-PNS modified by esmolol analogue(PAC-L-PNS)was prepared according to the optimal prescription,and its characterization,storage stability and characteristics of drug release in vitro were studied.Results:The optimal prescription and preparation of L-PNS were as follows:the mass ratio of phospholipid to cholesterol was 9:1,the ratio of drug to phospholipid was 1:20,the ultrasonic power was 63 W,the ultrasonic time was 10 min,the hydration time was 15min,and the concentration of drug was 1mg/mL.The particle size of PAC-L-PNS on the basis of optimal prescription was(222.70±2.55)nm,the Zeta potential was(+32.73±0.25)mV,and the entrapment efficiency and drug loading were 64.62%and 11.52%,respectively.The results of stability test showed that the leakage rates of L-PNS and PAC-L-PNS were both lower 30%within 48 hours,and there was no burst release phenomenon,indicating good stability;the in vitro release results showed that the cumulative release rates of L-PNS and PAC-LPNS in 72 h were 35.88%and 32.86%,respectively.Both of them were released smoothly without obvious burst release behavior and had a slow and controlled release effect.Conclusion:Based on the optimal prescription and preparation process,the PAC-L-PNS obtained by thin-film dispersion plus ultrasonic method has uniform particle distribution,positive surface charge,good dark-storage stability and slow release in vitro.

关 键 词：三七总皂苷 心肌靶向脂质体 制备工艺优化 质量评价 

分 类 号：R943[医药卫生—药剂学]