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    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-targeting liposomes of panax notoginseng saponins

      摘要
    • 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。

       

      Abstract: 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.

       

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